Herbicidal sulfonamides

ABSTRACT

Certain substituted pyrimidine sulfonylureas, such as 3-[[[(4-dimethoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester, are selective pre-emergence and/or post-emergence herbicides.

RELATED APPLICATION

This application is a division of U.S. Ser. No. 723,450, filed Apr. 15, 1985, which is a continuation of U.S. Ser. No. 543,835, filed Oct. 20, 1983, now abandoned, which is a continuation-in-part of U.S. Ser. No. 434,038, filed Oct. 20, 1982, now abandoned, which is a continuation-in-part of U.S. Ser. No. 328,018, filed Dec. 7, 1981, now abandoned.

BACKGROUND OF THE INVENTION

This invention relates to herbicidal sulfonamides, and, more particularly, to (dimethoxymethyl)pyrimidinyl sulfonylurea compounds which are selective pre-emergence and/or post-emergence herbicides.

DESCRIPTION OF THE PRIOR ART

U.S. Pat. Nos. 4,127,405 and 4,169,719 disclose herbicidal methoxymethylpyrimidine sulfonylurea compounds of the type which contain a --CH₂ OCH₃ heterocyclic substituent.

European Pat. No. 7687 discloses herbicidal sulfonylurea compounds such as, among others, ##STR1## where X is CH₃ or OCH₃ ;

Z is CH or N; and

Y is C₁ -C₄ alkyl substituted with OCH₃, OC₂ H₅, CN, C(O)L, or 1-3 atoms of F, Cl, or Br, where L is NH₂, OH, N(OCH₃)CH₃, NH(C₁ -C₄ alkyl), N(C₁ -C₄ alkyl) or C₁ -C₆ alkoxy.

U.S. application Ser. No. 116,920, discloses herbicidal substituted benzenesulfonylureas which contain as the heterocyclic substituent ##STR2## where X is CH₃ or OCH₃ ;

Z is CH or N; and

Y is (among others) C₁ -C₄ alkyl substituted with OC₂ H₅, CN, CO₂ H, CO₂ H₃ or CO₂ C₂ H₅.

J. Am. Chem. Soc., 69, 3072 (1947) teaches compounds of the formula: ##STR3## where A is H or ##STR4## X is Cl, CH₃, CH₃ O, CH₂ OCH₃, or H; and Y is CH(OCH₃)₂ or CH(OC₂ H₅)₂ ;

and their use as antibacterial agents.

SUMMARY OF THE INVENTION

This invention relates to novel compounds of Formula I, suitable agricultural compositions containing them, and their method of use as general and/or selective pre-emergence and/or post-emergence herbicides or plant growth regulants. ##STR5## wherein X is CH₃, OCH₃, Cl, C₂ H₅ or OC₂ H₅ ;

Z is CH or N;

Y is CH₂ OR, CH₂ S(O)_(m) R₁, CH(QR₁)₂, R₁ CHS(O)_(m) R₁, ##STR6## R is H, C(O)R₃, CO₂ R₄, C(O)NR₅ R₆ or ##STR7## R₁ is C₁ -C₂ alkyl; R₂ is --CH₂ CH₂ --, --CH(CH₃)CH₂ -- or --CH₂ CH₂ CH₂ --;

R₃ is C₁ -C₃ alkyl;

R₄ is C₁ -C₃ alkyl;

R₅ is H or CH₃ ;

R₆ is C₁ -C₃ alkyl;

Q is O or S;

m is 0, 1 or 2;

A is ##STR8## R₇ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, I, Br, NO₂, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₂, S(O)_(n) R₁₃, LCF₃, LCHF₂, LCF₂ CF₂ H, CH₂ Cl, CHCl₂, CH₂ OCH₃ or CH₂ OCH₂ CH₃ ;

R₈ is H, F, Cl, Br, CF₃, NO₂, C₁ -C₃ alkyl C₁ -C₃ alkoxy, OCF₂ H or SCF₂ H;

R₉ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ Cl or CH₂ CH═CH₂ ;

R₁₀ and R₁₁ are independently C₁ -C₃ alkyl;

R₁₂ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ CH₂ OCH₃ or C₁ -C₄ alkyl substituted with 1-3 atoms of F, Cl or Br;

R₁₃ is C₁ -C₄ alkyl or CH₂ CH═CH₂ ;

n is 0 or 2;

L is O, S or SO₂ ;

R₁₄ is H, CH₃, OCH₃, F, Cl, Br, NO₂, SO₂ N(CH₃)₂, OSO₂ R₁ or S(O)_(n) R₁ ;

R₁₅ is H, Cl, Br, CH₃, OCH₃ or NO₂ ;

R₁₆ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ;

R₁₇ is H, F, Cl, Br, CH₃ or OCH₃ ;

W is O or S;

W₁ is O or S;

R₁₈ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, NO₂, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ;

R₁₉ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, SO₂ NR₁₀ R₁₁, OSO₂ R₁₂, S(O)_(n) R₁₃, C₁ -C₃ alkyl, or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F;

R₂₀ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, C₁ -C₃ alkyl, OSO₂ R₁₂ or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F;

R₂₁ is H or CH₃ ;

and their agriculturally suitable salts; provided that

(1) the total number of carbon atoms of R₁₀ and R₁₁ is less than or equal to 4;

(2) when X is Cl, then Z is CH;

(3) when W is O, then R₁₈ is H, Cl, Br, CH₃ or CO₂ R₉ ;

(4) when W is O and R₁₈ is H, Cl, Br, or CH₃, then A is ##STR9## and (5) when W₁ is S, then R₂₁ is H and A is ##STR10##

Preferred for their higher herbicidal activity and/or more favorable ease of synthesis are:

(1) Compounds of Formula I where W₁ is O, X is CH₃, OCH₂ CH₃ or OCH₃ and R₂₁ is H;

(2) Compounds of Preferred 1 where Y is CH(QR₁)₂, CH₂ SR₁, CR₁ (QR₁)₂, ##STR11## (3) Compounds of Preferred 2 where Y is CH(QR₁)₂, CH₂ SR₁ or ##STR12## and Q is O; (4) Compounds of Preferred (3) wherein

A is ##STR13## R₇ is C₁ -C₃ alkyl, C₁ -C₃ alkoxy, Cl, NO₂, CO₂ R₉, SO₂ (C₁ -C₃ alkyl), SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₃, CH₂ OCH₃ or LCF₂ H;

R₁₄ is CH₃, OCH₃, Cl, OSO₂ CH₃ or SO₂ (C₁ -C₃ alkyl);

R₁₆ is CH₃, OCH₃, Cl, SO₂ CH₃ or SO₂ N(CH₃)₂ ;

R₁₈ is CH₃, Cl, Br, CO₂ R₉ or SO₂ CH₃ ;

(5) Compounds of Preferred (4) where A is ##STR14## and (6) Compounds of Preferred (5) where

R₇ is CO₂ CH₃, CO₂ CH₂ CH₃, SO₂ CH₃, SO₂ CH₂ CH₃, SO₂ N(CH₃)₂, OSO₂ CH₃, OSO₂ CH₂ CH₃ ; and

R₈ is H, F, Cl, CF₃, CH₃ or OCH₃.

Specifically preferred are:

3-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester;

2-chloro-N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]benzenesulfonamide;

2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]-2-methylsulfonylbenzenesulfonamide;

N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]-2-nitrobenzenesulfonamide;

2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, 2-propyl ester;

2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)pyrimin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[[4-(hydroxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[[4-(acetyloxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

5-chloro-2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

5-chloro-2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester; and

2-[[(4-(1,3-dioxolan-2-yl)-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.

The compounds of this invention are highly active pre-emergence and/or post-emergence herbicides. Certain compounds of this invention are useful for selective weed control in crops such as cotton, soybeans, wheat or corn.

DETAILED DESCRIPTION OF THE INVENTION Synthesis

The compounds of Formula I may be prepared by the reaction of an appropriately substituted sulfonyl isocyanate of Formula II with an appropriate 2-aminoheterocycle of Formula III according to Equation 1: ##STR15## wherein A, X, R₂₁ and Z(O)_(m) are as previously defined;

Y is CH₂ OR, CH₂ SR₁, CH(QR₁)₂ CH(QR₂ Q), CH(R₁)S(O)_(m) R₁, C(R₁)(QR₁)₂ or C(R₁)(QR₂ Q);

R is ##STR16## and m, R₁ and R₂ are as previously defined.

The reaction of Equation 1 is best carried out in an inert aprotic solvent such as methylene chloride, tetrahydrofuran, acetonitrile at a temperature between 20° and 80°. A catalytic amount of DABCO (1,4-diazabicyclo[2.2.2]octane) may be used to accelerate the reaction. In the cases in which the products are insoluble in the reaction solvent, they may be isolated by simple filtration. When the products are soluble in the reaction solvent they are isolated by evaporation of the solvent and trituration of the residue with solvents such as 1-chlorobutane, ethyl ether or methanol and filtration.

Preparation of isocyanates (II) is described in the following: U.S. Pat. No. 4,127,405, U.S. Pat. No. 4,169,719, Eur. Pat. No. 7,687, Eur. Pat. No. 13,480, Eur. Pat. No. 23,141, Eur. Pat. No. 23,422, Eur. Pat. No. 30,141, and Brit. 2,065, 116-A, the disclosures of which are herein incorporated by reference. Furthermore, the sulfonyl isocyanates of Formula IIa, which are disclosed in European Patent Pub. 44,212, may be prepared analogously to the teachings of U.S. Pat. No. 4,127,405. ##STR17## wherein R₈ and R₁₂ are as previously defined.

Certain compounds of Formula III are known in the art. For example, the compounds IIIa shown below: ##STR18## wherein X=CH₃, Cl or OCH₃ ; and

R₁ =CH₃ or C₂ H₅ ;

are described by W. Braker, et al., J. Amer. Chem. Soc., 69, 3072 (1947), the disclosures of which are herein incorporated by reference.

Triazines of Formula IIIb may be prepared according to the methods outlined in Equations 2 and 3. ##STR19## wherein R₁ and R₂ are as previously defined; and

Y is as defined in Equation 1, with m=0 or 2.

The reaction of Equation 2a is carried out according to the teachings of J. M. McElvain and R. L. Clarke, J. Amer. Chem. Soc., 69, 2657 (1947), in which the preparation of ethyl diethoxyiminoacetate is described. The intermediate N-cyanoimidates of Formula VI may be prepared according to the teaching of D. Lwowski in Synthesis, 1971, 263, by reacting V with cyanamide at pH 5.5, and these may be condensed according to reaction 2c with the appropriate compound of Formula VII in an alcoholic solvent at 25° to 80° C. to provide the appropriate triazines. Alternatively, the reaction of Equation 3a, described for substituted acetonitriles by F. C. Schaefer and G. A. Peters in J. Org. Chem., 26, 412 (1961), may be used to convert nitriles of Formula IV to the corresponding iminoesters. The free base may be carried on through reactions 2b and 2c, or, alternatively, converted to the amidinium hydrochloride salts (VIII) as described in the aforementioned reference. The compounds of Formula VIII may be converted to the compounds IIIb by the reaction of Equation 3c, in which VIII is contacted with a compound of Formula IX at 0° to 30° C. in the presence of 3-4 equivalents of the appropriate sodium alkoxide in the appropriate alcohol. The product may be isolated by evaporation of solvent, neutralization with aqueous acetic acid, and filtration. ##STR20## wherein Y is as defined in Equation 1 with m=0;

X is R₁ or SCH₃ ; and

R₁ and R₂ are as previously defined.

The compounds of Formula IIIc may be prepared by the sequence of reactions outlined in Equation 4. ##STR21## wherein Y, m, R₁ and R₂ are as defined in Equation 3.

The reactions of Equations 4a and 4b are carried out as described by W. Braker, et al., loc. cit.

The compounds of Formula IIId may be prepared by similar methods shown in Equation 5. ##STR22## wherein R₂₁, R₁ and Y are as defined in Equation 1.

The reactions of Equations 5a and 5b are conducted as described for 2-amino-4-hydroxy-6-dimethoxymethylpyrimidine (J. I. De Graw and V. H. Brown, J. Het. Chem., 13, 439 (1976)). The silver salt of XIII may be prepared by addition of ammonia to an aqueous solution of XIII and an equivalent amount of silver nitrate. The dried silver salt may be contacted with one equivalent of methyl or ethyl iodide in a nonpolar solvent such as benzene at 25° to 80° C. to provide pyrimidines of Formula IIId after purification by column chromatography or recrystallization.

Alternatively, the compounds of Formula IIId may be prepared via the corresponding chloropyrimidines (IIIe). These may be obtained by the reaction of Equation 6a, in which a compound of Formula XIII is contacted with 2-5 equivalents of phosphorous oxychloride at 20°-90° C. for 3-30 hours. The product is isolated by removal of excess POCl₃ in vacuo, treatment of the residue with ice-water, extraction into an organic solvent, concentration, crystallization or column chromatography. The chloropyrimidines may then be converted to the compounds of Formula IIId by contacting with one equivalent of the appropriate sodium alkoxide in alcohol at 0°-30° C. followed by concentration and precipitation with ice-water. ##STR23## wherein Y is CH(QR₁)₂, CH₂ SR₁, CH(QR₂ Q), C(R₁)(QR₁)₂, CH(R₁)S(O)_(m) R₁ or C(R₁)(QR₂ Q);

R₁, R₂ and R₂₁ are as defined in Equation 1; and

m=0 or 2.

The ketoesters of Formula XII may be prepared by the methods of Equation 7. ##STR24## wherein m, Y and R₁ are as defined in Equation 3.

The reaction of Equation 7a is carried out by the slow addition of the appropriate dialkyl carbonate to a solution of the appropriate methyl ketone of Formula XV in an inert solvent (such as toluene) at 30°-110° in the presence of 1-2 equivalents of sodium hydride. The product may be isolated by concentration, neutralization, and extraction from water into an organic solvent, such as diethyl ether. The product may then be purified by distillation. Compounds of Formula XIIa may be obtained by the well-known reaction of a γ-chloroacetoacetic ester (XVI) with the appropriate sodium mercaptide or alkylsulfinate in a hydroxylic or dipolar aprotic solvent.

Cyclic acetals of formula IIIe may be prepared from compounds of Formula IIIa according to Equation 8 by acetal exchange. ##STR25## wherein X, Q, Z, R₁ and R₂ are defined in Equation 1; and

R₂₂ is H, CH₃ or C₂ H₅.

The reaction of Equation 8 is carried out by heating the acyclic acetal in a inert solvent in the presence of one equivalent of a compound of Formula XVII and slightly more than one equivalent of an acidic catalyst, such as p-toluenesulfonic acid or boron trifluoride etherate with distillation of the by-product alcohol. The compound of Formula IIIe may be isolated by extraction with an organic solvent, and purified by crystallization or column chromatography.

The synthesis of N-methyl compounds of Formula IIIg may be accomplished by the procedure shown in Equation 9. ##STR26## wherein Z, R₁ and Q are as previously defined;

Y is as defined in Equation 1; and

X is CH₃, C₂ H₅, OCH₃ or OC₂ H₅.

The reaction of Equation 9a may be carried out by stirring a mixture of IIIf with one equivalent each of sodium hydride and dimethyl carbonate for 1-3 days in an inert solvent such as tetrahydrofuran or dimethylformamide. The product of Formula XVIII may be isolated by evaporation of solvent, neutralization with aqueous acetic acid, and filtration of the product. The reaction of Equation 8b is performed by adding XVI to a slurry of one equivalent of sodium hydride in tetrahydrofuran at 0°-30°, stirring for 1/2 hour, and adding methyl iodide, heating to reflux for 1-20 hours, and stirring with water and aqueous sodium hydroxide for 1-20 hours at 20°-30°. The product is isolated by evaporating the solvent, adding ice-water, and filtering.

The acetals and ketals of Formula IIIi may be prepared from the corresponding thioethers of Formula IIIh by the reaction of Equation 10. ##STR27## wherein X, R₁, R₂₁ and Z are as previously defined; and

R₂₂ is H, CH₃ or C₂ H₅.

The reaction of Equation 10 may be carried out by adding 2 to 2.3 equivalents of N-chlorosuccinimide to an alcoholic solution of a sulfide of Formula IIIh in the presence of 0.01 to 0.2 equivalents of a strong acid, such as H₂ SO₄, at -20° to 20° C. After 10 to 100 minutes, the reaction mixture is concentrated, diluted with water, and the reaction product is isolated by crystallization or extraction into an organic solvent.

Thioacetals and thioketals of Formula IIIj may be prepared by the reaction of Equation 11. ##STR28## wherein X is CH₃, C₂ H₅, OCH₃ or OC₂ H₅ ; and

Z, R₁, R₂₁ and R₂₂ are as defined in Equation 10.

The reaction of Equation 11a may be carried out by contacting a carbamate of Formula XVIIIa with 2-2.5 equivalents of lithium diisopropylamide in a solvent such as tetrahydrofuran at -78° and then with 1 to 2 equivalents of the appropriate dialkyl disulfide and allowing the mixture to warm to 20°. The product of Formula XVIIIb may be isolated by concentration, neutralization, and extraction into an organic solvent. Purification may be accomplished by column chromatography or recrystallization. The reaction of Equation 11b is carried out by contacting with aqueous alkali for 10-100 minutes at 20°-80° and extracting the product into an organic solvent. The product may be isolated by concentration and crystallization.

The preparation of compounds of Formula IIIk is shown in Equation 12. ##STR29## wherein Z, R₁ and X are as defined in Equation 11.

The reaction of Equation 12a is carried out as described for Equation 11a, only using one equivalent of the appropriate alkyl iodide, rather than a disulfide. The reaction of Equation 12b is carried out as described for Equation 11b.

Sulfoxides and sulfones of Formula IIIl and IIIo, respectively, may be prepared from the corresponding sulfides of Formula IIIh as shown in Equation 13. ##STR30## wherein Z, X, R₁, R₂₁ and R₂₂ are as defined in Equation 10.

The reaction of Equation 13a is carried out by contacting IIIh with 0.9 to 1.1 equivalents of m-chloroperbenzoic acid in an inert solvent at -20° to 0° for 1 to 2 hours, concentration, and trituration with ether. If the product is ether-soluble, it is isolated by washing an ether solution with aqueous bicarbonate and concentration of the dried ether phase. The preparation of the corresponding sulfones is accomplished in the same way except that 2 to 2.2 equivalents of MCPBA are used at 0°-30° for 1-24 hours.

Compounds of Formula Ib may be prepared by acidic hydrolysis of compounds of Formula Ia according to Equation 14: ##STR31## wherein A, X, R₂₁ and Z are as defined in Equation 1.

The reaction of Equation 14 is carried out by stirring a solution or suspension of Ia in aqueous acetone containing a catalytic amount of a strong mineral acid, such as hydrochloric or sulfuric acid, at 0° to 30° C., followed by concentration and filtration of the product.

The compounds of Formula Ib may be in turn converted to compounds of Formulae Ic, Id, or Ie according to Equation 15: ##STR32## wherein A, X, Z, R₃, R₄, R₅, R₆ and R₂₁ are as previously defined.

The reactions of Equation 15 are carried out by contacting a compound of Formula Ib with at least one equivalent of an alkyl carboxylic anhydride, carbonyl chloride, chloroformate or carbamoyl chloride in an inert solvent in the presence of an excess of an acid acceptor such as pyridine, triethylamine, or aqueous sodium carbonate, followed by isolation of the product by acidification and crystallization or extraction into an organic solvent. Alternatively, compounds of Formula Ie wherein R₅ =H may be prepared by contacting the appropriate compound of Formula Ib with one equivalent of an appropriate alkyl isocyanate in an inert solvent and filtration of the product.

Certain compounds of Formula I may also be prepared by the reactions of Equation 16. ##STR33## wherein R₂₁, X and A are as previously defined, provided that R₇, R₁₆, R₁₈ and R₁₉ are not CO₂ R₉.

The reaction of Equation 16a is conducted in the same manner as described for Equation 1. The resulting compounds of Formula XIX may be converted to compounds of Formula If by contacting them with 3-5 equivalents of diisobutyl aluminum hydride in an ethereal solvent at -20° to 20°, after which the reaction mixture is quenched with aqueous mineral acid and extracted with an organic solvent. The product may be isolated by evaporation of solvent and crystallization.

Equation 17 outlines the preparation of the compounds of Formula XX. ##STR34## wherein R₁ and R₂₁ are as previously defined.

The pyrimidine of Formula XXII is described by Z. Budesinsky and F. Roubinek, in Coll. Czech. Chem. Comm., 26, 2871 (1961). This may be heated in an autoclave at 80° to 140° with ammonia or methyl amine to afford the amino acids of Formula XXIII. These may be esterified in the usual manner with methanol and acid, followed by evaporation of solvent, neutralization and filtration to afford the compounds of Formula XXa.

The preparation of XXb (R₂₁ =H) is reported in J. Org. Chem., 26, 2755, by G. Davies, et al., and the N-methyl compounds (R₂₁ =CH₃) may be prepared in an analogous fashion. The reaction of Equation 17c is conducted according to the procedure described for Equation 6b.

EXAMPLE 1 2-Amino-4-(dimethoxymethyl)-6-methylpyrimidine

To 6.9 g of sodium pellets in 120 ml of toluene containing 50 g of methyl dimethoxyacetate was added 20 g of acetone dropwise over 30 minutes at 0°-20°. The mixture was stirred overnight at room temperature, concentrated at reduced pressure, and the product was precipitated with ether and filtered. Ten ml of acetic acid in ice-water was added, and the β-diketone was extracted with methylene chloride. The residue from concentration of the organic extract was heated with 25 g of guanidine carbonate at 80°-90° for 30 minutes, cooled, digested with methylene chloride, filtered, dried with sodium sulfate, filtered, concentrated at reduced pressure, and triturated with petroleum ether to provide 11 g of 2-amino-4-dimethoxymethyl-6-methylpyrimidine, m.p. 69°-71° (lit, m.p. 71°-74°).

NMR (CDCl₃)δ: 2.3 (s, 3), 3.3 (s, 6), 5.0 (s, 1), 5.9 (br s, 2), 6.7 (s, 1).

EXAMPLE 2 2-Chloro-N-[[4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]benzenesulfonamide

A solution of 0.3 g of 2-amino-4-dimethoxymethyl-6-methylpyrimidine in 50 ml of ether was stirred overnight at room temperature with 0.46 g of o-chlorobenzenesulfonyl isocyanate. The product was filtered and washed with hexane to provide 0.5 g of the title compound, m.p. 150°-153°.

NMR (CDCl₃)δ: 2.5 (s, 3), 3.4 (s, 6), 5.2 (s, 1), 7.1 (s, 1), 7.4 (m, 3), 7.9 (br s, 1), 8.3 (m, 1).

EXAMPLE 3 2-Amino-4-methyl-6-(tetrahydropyran-2-yloxymethyl)pyrimidine

A solution containing 30 g of methyl glycolate, 33 g of dihydropyran, and 0.2 g of p-toluenesulfonic acid in 100 ml of toluene was stirred at room temperature overnight. After cooling to -5°, 6.8 g of sodium pellets was added, followe by 24 ml of acetone at -5° to 8°. Stirring was continued for 20 hours at room temperature, after which time hexane was added, and the solution was poured into ice-water and partitioned. The aqueous phase was washed with ether and acidified with 20 ml of acetic acid, extracted with 600 ml of methylene chloride, the organic layer was dried (MgSO₄) and concentrated, and the residue was heated at 80°-90° with 28 g of guanidine carbonate for 1 hour. Addition of ice-water to the cooled reaction mixture precipitated the product, which was filtered and dried to afford the title compound, m.p. 109°-110.5°.

NMR (CDCl₃)δ: 1.7 (br s, 6), 2.3 (s, 3), 3.6 (br m, 2), 4.5 (d, 2), 4.7 (m, 1), 5.4 (br s, 2), 6.6 (br s, 1).

EXAMPLE 4 Methyl 2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)pyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoate

To a solution of 3.25 g of the product from Example 3 in 50 ml of ether was added 3.75 g of 2-methoxycarbonylbenzenesulfonyl isocyanate and the mixture was stirred for 3 hours under nitrogen. The precipitated product was filtered and washed with ether to afford 6.0 g of the title compound, m.p. 126°-128° (d).

EXAMPLE 5 Methyl [[[4-(hydroxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoate

A solution of 6 g of the product prepared in Example 4 in 50 ml of acetone was stirred with 3 ml of 1N aqueous HCl for 3 days at room temperature, concentrated at reduced pressure, and the residue was thoroughly washed with water to provide 4 g of the title compound, m.p. 140°-141°.

NMR (CDCl₃ +DMSO-d₆)δ: 2.5 (s, 3), 3.9 (s, 3), 4.6 (br s, 2), 7.0 (br s, 1), 7.6 (m, 3), 8.3 (m, 1), 9.6 (br s, 1).

EXAMPLE 6 Methyl [[[4-(acetoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoate

To 0.5 g of the compound from Example 5 was added 1 ml of acetic anhydride and 1 ml of pyridine. After 1 hour at room temperature, ice-water was added, the precipitated oil was triturated, filtered, and washed with water to afford 0.4 g of the title compound, m.p. 145°-150°.

NMR (CDCl₃)δ: 2.2 (s, 3), 2.6 (s, 3), 3.9 (s, 3), 5.2 (s, 2), 6.9 (s, 1), 7.7 (m, 3), 8.3 (br s, 1), 8.4 (m, 1), 13.1 (br s, 1).

                                      TABLE 1a                                     __________________________________________________________________________      ##STR35##                                                                     R.sub.7    R.sub.8                                                                              R.sub.21                                                                           X     Y         m.p. (°C.)                         __________________________________________________________________________     Cl         H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                      150-153°                           CO.sub.2 CH.sub.3                                                                         H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                      121-125°                           SO.sub.3 CH.sub.3                                                                         H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                      152-155°                           NO.sub.2   H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                      144-152°                           CO.sub.2 CH(CH.sub.3).sub.2                                                               H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                       73-79°                            CO.sub.2 C.sub.2 H.sub.5                                                                  H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CF.sub.3   H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 Br         H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CH.sub.3   H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 C.sub.2 H.sub.5                                                                           H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                      135-145° d                         SO.sub.2 N(CH.sub.3).sub.2                                                                H     H   CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                                                      146-157°                           OCH.sub.3  6-OCHF.sub.2                                                                         H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 OCF.sub.2 CF.sub.2 H                                                                      H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CH.sub.2 OCH.sub.3                                                                        H     H   CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                 OSO.sub.2 CHCl.sub.2                                                                      H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SC.sub.2 H.sub.5                                                                          H     H   CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                 OSO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 OSO.sub.2 C.sub.2 H.sub.5                                                                 H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                      H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 C.sub.2 H.sub.5                                                                  H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 NO.sub.2   5-CF.sub.3                                                                           H   CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               3-Cl  H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 OC.sub.2 H.sub.5                                                                          5-NO.sub.2                                                                           H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 C.sub.2 H.sub.5                                                                  H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                       98-100° d                         I          H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                       6-NO.sub.2                                                                           H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 Cl         5-Cl  H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                         5-Cl  H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 CH.sub.3                                                                         4-F   H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 OCH.sub.2 CHCH.sub.2                                                                      H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CH(OCH.sub.3)CH.sub.3                                                                     H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 CF.sub.3                                                                         H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SCHF.sub.2 H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 OCH.sub.2 CHCHCH.sub.3                                                                    H     H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 Cl         H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 CH.sub.3                                                                         H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub. 2                                CO.sub.2 CH.sub.2 CH.sub.3                                                                H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                         H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CH(CH.sub.3).sub.2                                                                        H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 OCH.sub.3  H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SCH.sub.3  H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                  -n-C.sub.4 H.sub.9                                                                       H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 O -n-C.sub.4 H.sub.9                                                                      H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 NO.sub.2   H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 -n-C.sub.4 H.sub.9                                                               H     CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 Cl         H     H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        CH.sub.2 OCH.sub.3                                                                        H     H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        SO.sub.2 C.sub.2 H.sub.5                                                                  H     H   CH.sub.3                                                                             C(CH.sub.3 )(OCH.sub.3).sub.2                       OCH.sub.3  H     H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        SC.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        CO.sub.2 C.sub.2 H.sub.5                                                                  H     H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        CO.sub.2 CH.sub.3                                                                         5-Cl  H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        Cl         H     H   CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                 CO.sub.2 CH.sub.3                                                                         H     H   CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                         H     H   CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                 NO.sub.2   H     H   CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                 __________________________________________________________________________

                  TABLE 1b                                                         ______________________________________                                          ##STR36##                                                                                                             m.p.                                   R.sub.7     R.sub.8  R.sub.21X  Y       (°C.)                           ______________________________________                                         NO.sub.2    H        HCH.sub.3  CH.sub.2 OTHP                                                                          129-                                                                           132°                            Br          H        HCH.sub.3  CH.sub.2 OTHP                                  Cl          H        HCH.sub.3  CH.sub.2 OTHP                                                                          148-                                                                           150°                            SO.sub.2 CH.sub.3                                                                          H        HCH.sub.3  CH.sub.2 OTHP                                                                          161-                                                                           165°                            F           H        HCH.sub.3  CH.sub.2 OTHP                                  H           H        HCH.sub.3  CH.sub.2 OTHP                                  CO.sub.2 CH.sub.3                                                                          H        HCH.sub.3  CH.sub.2 OTHP                                                                          126-                                                                           128°                            CH.sub.3    5-SCHF.sub.2                                                                            HCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                 H        HCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                                H        HCH.sub.3  CH.sub.2 OTHP                                  OCH.sub.3   H        HCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  O -n-C.sub.3 H.sub.7                                                                       H        HCH.sub.3  CH.sub.2 OTHP                                  CH.sub.2 OCH.sub.3                                                                         H        HCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H        HCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                 H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  OC.sub.2 H.sub.5                                                                           H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  CO.sub.2 Et H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  OCF.sub.2 CF.sub.2 H                                                                       H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  CH.sub.2 OCH.sub.3                                                                         H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  Cl          H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  SC.sub.2 H.sub.5                                                                           H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OTHP                                  SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H        HCH.sub.3  CH.sub.2 OTHP                                  SCF.sub.3   H        HCH.sub.3  CH.sub.2 OTHP                                  CH(OCH.sub.3)CH.sub.3                                                                      H        HCH.sub.3  CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 1c                                                         ______________________________________                                          ##STR37##                                                                                                             m.p.                                   R.sub.7      R.sub.8  R.sub.21 X Y      (°C.)                           ______________________________________                                         Cl           H        HCH.sub.3  CH.sub.2 OH                                                                           130-                                                                           132°                            CO.sub.2 CH.sub.3                                                                           H        HCH.sub.3  CH.sub.2 OH                                                                           140-                                                                           141°                            SO.sub.2 CH.sub.3                                                                           H        HCH.sub.3  CH.sub.2 OH                                                                           155°                                                                    d                                      NO.sub.2     H        HCH.sub.3  CH.sub.2 OH                                                                           112-                                                                           116°                            CO.sub.2 CH(CH.sub.3).sub.2                                                                 H        HCH.sub.3  CH.sub.2 OH                                                                           154-                                                                           157°                            CO.sub.2 C.sub.2 H.sub.5                                                                    H        HCH.sub.3  CH.sub.2 OH                                   CF.sub.3     H        HCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                   Br           H        HCH.sub.3  CH.sub.2 OH                                   CH.sub.3     H        HCH.sub.3  CH.sub.2 OH                                   C.sub.2 H.sub.5                                                                             H        HCH.sub.3  CH.sub.2 OH                                   SO.sub.2 -n-C.sub.3 H.sub.7                                                                 H        HCH.sub.3  CH.sub.2 OH                                                                           128°                                                                    d                                      SO.sub.2 N(CH.sub.3).sub.2                                                                  H        HCH.sub.3  CH.sub.2 OH                                                                           163-                                                                           169°                                                                    d                                      OCH.sub.3    H        HCH.sub.3  CH.sub.2 OH                                   CO.sub.2 CH.sub.2 CHCH.sub.2                                                                H        HCH.sub.3  CH.sub.2 OH                                   OCF.sub.2 CF.sub.2 H                                                                        H        HCH.sub.3  CH.sub.2 OH                                   CH.sub.2 OCH.sub.3                                                                          H        HCH.sub.3  CH.sub.2 OH                                   OSO.sub.2 CHCl.sub.2                                                                        H        HCH.sub.3  CH.sub.2 OH                                   SC.sub.2 H.sub.5                                                                            H        HCH.sub.3  CH.sub.2 OH                                   OSO.sub.2 CH.sub.3                                                                          3-OCHF.sub.2                                                                            HCH.sub.3  CH.sub.2 OH                                   OSO.sub.2 C.sub.2 H.sub.5                                                                   H        HCH.sub.3  CH.sub.2 OH                                   CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                        H        HCH.sub.3  CH.sub.2 OH                                   SO.sub.2 C.sub.2 H.sub.5                                                                    H        HCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                   NO.sub.2     5-CF.sub.3                                                                              HCH.sub.3  CH.sub.2 OH                                   SO.sub.2 -n-C.sub.3 H.sub.7                                                                 3-Cl     HCH.sub.3  CH.sub.2 OH                                   OC.sub.2 H.sub.5                                                                            5-NO.sub.2                                                                              HCH.sub.3  CH.sub.2 OH                                   SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                         6-NO.sub.2                                                                              HCH.sub.3  CH.sub.2 OH                                   Cl           5-Cl     HCH.sub.3  CH.sub.2 OH                                   SO.sub.2 CH.sub.3                                                                           5-Cl     HCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                   CO.sub.2 CH.sub.3                                                                           4-F      HCH.sub.3  CH.sub.2 OH                                   NO.sub.2     H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   Br           H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   Cl           H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   SO.sub.2 CH.sub.3                                                                           H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   F            H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   H            H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   CO.sub.2 CH.sub.3                                                                           H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   CH.sub.3     H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                            H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   SCF.sub.3    H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   SO.sub.2 CH.sub.2 CHCH.sub.2                                                                H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   SCH.sub.2 CH.sub.3                                                                          H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   OCH.sub.2 CHCH.sub.2                                                                        H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   OCH.sub.2 C(CH.sub.3)CH.sub.2                                                               H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   CH.sub.2 OEt H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   CH(OCH.sub.3)CH.sub.3                                                                       H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                               H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   O .sub.-i-C.sub.3 H.sub.7                                                                   H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                    .sub.-i-C.sub.4 H.sub.9                                                                    H        CH.sub.3CH.sub.3                                                                          CH.sub.2 OH                                   SO.sub.2 Et  H        HCH.sub.3  CH.sub.2 OH                                    -n-C.sub.4 H.sub.9                                                                         H        HCH.sub.3  CH.sub.2 OH                                   O -n-C.sub.4 H.sub.9                                                                        H        HCH.sub.3  CH.sub.2 OH                                   O .sub.-t-C.sub.4 H.sub.9                                                                   H        HCH.sub.3  CH.sub.2 OH                                   SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                         H        HCH.sub.3  CH.sub.2 OH                                   I            H        HCH.sub.3  CH.sub.2 OH                                   OCF.sub.2 H  H        HCH.sub.3  CH.sub.2 OH                                   SCF.sub.2 CF.sub.2 H                                                                        H        HCH.sub.3  CH.sub.2 OH                                   CH.sub.2 Cl  H        HCH.sub.3  CH.sub.2 OH                                   ______________________________________                                    

                                      TABLE 1d                                     __________________________________________________________________________      ##STR38##                                                                     R.sub.7   R.sub.8                                                                               R.sub.21                                                                          X  Y            m.p. (°C.)                          __________________________________________________________________________     H         H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                H         H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           H         H      H  C.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                    H         H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                      H         H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    158-163°                            Cl        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                Cl        H      H  C.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                                Cl        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        6-Cl   H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        4-F    H  CH.sub.3                                                                          CH(OEt).sub.2                                           Cl        H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           CH.sub.3  H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           CH.sub.3  H      H  C.sub.2 H.sub.5                                                                   CH(OEt).sub.2                                           CH.sub.3  H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                      C.sub.2 H.sub.5                                                                          H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    C.sub.2 H.sub.5                                                                          H      CH.sub.3                                                                          CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    C.sub.2 H.sub.5                                                                          5-Cl   H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                     -n-C.sub.4 H.sub.9                                                                      H      H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             OCH.sub.3 H      H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             OCH.sub.3 3-NO.sub.2                                                                            H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             OCH.sub.3 H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCH.sub.3 H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           OSO.sub.2 CH.sub.3                                                                       H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       151-155°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       153-157°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       104-107°                            NO.sub.2  H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       133-138°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                                                        145-150°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                       CO.sub.2 CH.sub.3                                                                        H      H  C.sub.2 H.sub.5                                                                   CH(OEt).sub.2                                           CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 SEt                                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    151-156°                            CO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.3                                                                        6-CH.sub.3                                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.3                                                                        5-OEt  H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.3                                                                        4-CF.sub.3                                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 OCOEt                                          SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 OCOEt                                          SO.sub.2 CH.sub.3                                                                        3-F    H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                      SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    193-195° d                          SO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                        6-O -n-C.sub.3 H.sub.7                                                                H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                        3- .sub.-i-C.sub.3 H.sub.7                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH.sub.2 OCO -n-C.sub.3 H.sub.7                         SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(SCH(CH.sub.3)CH.sub.2 S)                             SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    185-187°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 N(CH.sub.3).sub.2                                                               6-NO.sub.2                                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  3-Br   H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  6-Cl   CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  H      H  C.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    179-182° d                          NO.sub.2  3-F    H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Br        H      H  CH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 S)                                Br        H      H  CH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                             CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    119-121°                            I         H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CH.sub.2 Cl                                                                              H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCHF.sub.2                                                                               H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                Br        H      CH.sub.3                                                                          CH.sub.3                                                                          CH.sub.2 OCONHCH.sub.3                                  CF.sub.3  H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CF.sub.3  H      H  CH.sub.3                                                                          CH.sub.2 SEt                                            SO.sub.2 N(Et).sub.2                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCH.sub.2 CH.sub.3                                                                       H      H  C.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                                O -n-C.sub.4 H.sub.9                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                O .sub.-i-C.sub.3 H.sub.7                                                                H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCH.sub.2 CHCH.sub.2                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CF.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CF.sub.3                                                                        5-CF.sub.3                                                                            H  CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 CF.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    144° d                              OCF.sub.2 CF.sub.2 H                                                                     H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    OCF.sub.2 CF.sub.2 H                                                                     H      H  C.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                    OCF.sub.2 CF.sub.2 H                                                                     H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    OSO.sub.2 C.sub.2 H.sub.5                                                                H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    CH.sub.2 OEt                                                                             6-F    H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H      H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             SO.sub.2 N(CH.sub.3)Et                                                                   H      H  CH.sub.3                                                                          CH.sub.2 OCO.sub.2 Et                                   SO.sub.2 N(CH.sub.3)Et                                                                   H      H  CH.sub.3                                                                          CH.sub.2 OCON(CH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3)Et                                                                   H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        H      H  CH.sub.3                                                                          CH(SEt).sub.2                                           CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          C(CH.sub.3)(SCH.sub.3).sub.2                            CO.sub.2 C.sub.2 H.sub.5                                                                 H      H  CH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                       NO.sub.2  H      H  CH.sub.3                                                                          C(C.sub.2 H.sub.5)(SCH.sub.2 CH.sub.2 CH.sub.2 S)       SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(CH.sub.3)SO.sub.2 CH.sub.3                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          179-185°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          133-138°                            Cl        H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          133-135°                            NO.sub.2  H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          148-154°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          127-133°                            Cl        H      H  CH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.3                                                                  182-187°                            Cl        H      H  CH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                   SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(CH.sub.3)(S(O)CH.sub.3)                              NO.sub.2  H      H  CH.sub.3                                                                          CH(CH.sub.3)(SO.sub.2 CH.sub.3)                         Cl        H      H  CH.sub.3                                                                          CH.sub.2 S(O)CH.sub.2 CH.sub.3                          CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                     SO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  CH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                   __________________________________________________________________________

                                      TABLE 1e                                     __________________________________________________________________________      ##STR39##                                                                     R.sub.7   R.sub.8                                                                            R.sub.21                                                                          X     Y        m.p. (°C.)                              __________________________________________________________________________     Cl        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     179-182°                                CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     121-133°                                SO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     162° d                                  NO.sub.2  H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     150° d                                  CO.sub.2 CH(CH.sub.3).sub.2                                                              H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 C.sub.2 H.sub.5                                                                 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CF.sub.3  H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Br        H   CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.3  H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                          H   H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     161-167° d                              SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                      93-102° d                              OCH.sub.3 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCF.sub.2 CF.sub.2 H                                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.2 OCH.sub.3                                                                       H   H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CHCl.sub.2                                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SC.sub.2 H.sub.5                                                                         H   CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 C.sub.2 H.sub.5                                                                H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 C.sub.2 H.sub.5                                                                 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  5-CF.sub.3                                                                         H  OCH.sub. 3                                                                           CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              3-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OC.sub.2 H.sub.5                                                                         5-NO.sub.2                                                                         H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.2 CH.sub.3                                                               H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      6-NO.sub.2                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        5-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        5-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        4-F H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     __________________________________________________________________________

                  TABLE 1f                                                         ______________________________________                                          ##STR40##                                                                     R.sub.7     R.sub.8                                                                               R.sub.21 X                                                                               Y       m.p. (°C.)                         ______________________________________                                         NO.sub.2    H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     Br          H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     Cl          H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     SO.sub.2 CH.sub.3                                                                          H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     F           H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     H           H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     CO.sub.2 CH.sub.3                                                                          H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     CH.sub.3    H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     SO.sub.2 N(CH.sub.3).sub.2                                                                 H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                                H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     OCH.sub.3   H      HOCH.sub.3                                                                               CH.sub. 2 OTHP                                    O -n-C.sub.3 H.sub.7                                                                       H      CH.sub.3 OCH.sub.3                                                                       CH.sub.2 OTHP                                     CH.sub.2 OCH.sub.3                                                                         H      CH.sub.3 OCH.sub.3                                                                       CH.sub.2 OTHP                                     CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     Cl          6-Cl   HOCH.sub.3                                                                               CH.sub.2 OTHP                                     I           H      HOCH.sub.3                                                                               CH.sub.2 OTHP                                     ______________________________________                                    

                  TABLE 1g                                                         ______________________________________                                          ##STR41##                                                                                                            m.p.                                    R.sub.7     R.sub.8 R.sub.21 X  Y      (°C.)                            ______________________________________                                         Cl          H       HOCH.sub.3  CH.sub.2 OH                                    CO.sub.2 CH.sub.3                                                                          H       HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 CH.sub.3                                                                          H       HOCH.sub.3  CH.sub.2 OH                                                                           170° d                           NO.sub.2    H       HOCH.sub.3  CH.sub.2 OH                                    CO.sub.2 CH(CH.sub.3).sub.2                                                                H       HOCH.sub.3  CH.sub.2 OH                                    CO.sub.2 C.sub.2 H.sub.5                                                                   H       HOCH.sub.3  CH.sub.2 OH                                    CF.sub.3    H       HOCH.sub.3  CH.sub.2 OH                                    Br          H       HOCH.sub.3  CH.sub.2 OH                                    CH.sub.3    H       CH.sub.3 OCH.sub.3                                                                         CH.sub.2 OH                                    C.sub.2 H.sub.5                                                                            H       HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 N(CH.sub.3).sub.2                                                                 H       HOCH.sub.3  CH.sub.2 OH                                    OCH.sub.3   H       HOCH.sub.3  CH.sub.2 OH                                    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                    OCF.sub.2 CF.sub.2 H                                                                       H       HOCH.sub.3  CH.sub.2 OH                                    CH.sub.2 OCH.sub.3                                                                         H       HOCH.sub.3  CH.sub.2 OH                                    OSO.sub.2 CHCl.sub.2                                                                       H       HOCH.sub.3  CH.sub.2 OH                                    SC.sub.2 H.sub.5                                                                           H       CH.sub.3 OCH.sub.3                                                                         CH.sub.2 OH                                    OSO.sub.2 CH.sub.3                                                                         H       HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                    OSO.sub.2 C.sub.2 H.sub.5                                                                  H       HOCH.sub.3  CH.sub.2 OH                                    CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 C.sub.2 H.sub.5                                                                   H       HOCH.sub.3  CH.sub.2 OH                                    NO.sub.2    5-CF.sub.3                                                                             HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 -n-C.sub.3 H.sub.7                                                                3-Cl    HOCH.sub.3  CH.sub.2 OH                                    OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             HOCH.sub.3  CH.sub.2 OH                                    I           H       HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             HOCH.sub.3  CH.sub.2 OH                                    Cl          5-Cl    HOCH.sub.3  CH.sub.2 OH                                    SO.sub.2 CH.sub.3                                                                          5-Cl    HOCH.sub.3  CH.sub.2 OH                                    CO.sub.2 CH.sub.3                                                                          4-F     HOCH.sub.3  CH.sub.2 OH                                    ______________________________________                                    

                                      TABLE 1h                                     __________________________________________________________________________      ##STR42##                                                                     R.sub.7   R.sub.8                                                                               R.sub.21                                                                          X   Y           m.p. (°C.)                          __________________________________________________________________________     H         H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               H         H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          H         H      H  OC.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                   H         H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                     H         H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   105-112° d                          Cl        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               Cl        H      H  OC.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                               Cl        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        6-Cl   H  OCH.sub.3                                                                          OCH(OCH.sub.2 CH.sub. 2 CH.sub.2 O)                    Cl        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        4-F    H  OCH.sub.3                                                                          CH(OEt).sub.2                                          Cl        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              143-145°                            CH.sub.3  H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          CH.sub.3  H      H  OC.sub.2 H.sub.5                                                                   CH(OEt).sub.2                                          CH.sub.3  H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                     C.sub.2 H.sub.5                                                                          H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   C.sub.2 H.sub.5                                                                          H      CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   C.sub.2 H.sub.5                                                                          5-Cl   H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    -n-C.sub.4 H.sub.9                                                                      H      H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            OCH.sub.3 H      H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            OCH.sub.3 3-NO.sub.2                                                                            H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            OCH.sub.3 H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCH.sub.3 H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   145-149°                            Cl        H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      C.sub.2 H.sub.5                                                                          H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              127-144°                            CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SEt                                           CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   161-163°                            CO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.3                                                                        6-CH.sub.3                                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.3                                                                        5-OEt  H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.3                                                                        4-CF.sub.3                                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 OCOEt                                         SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              210-213°                            SO.sub.2 CH.sub.3                                                                        3-F    H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                     SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        6-O -n-C.sub.3 H.sub.7                                                                H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        3- .sub.-i-C.sub.3 H.sub.7                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH.sub.2 OCO -n-C.sub.3 H.sub.7                        SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              138-141°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH(SCH(CH.sub.3)CH.sub.2 S)                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 N(CH.sub.3).sub.2                                                               H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 N(CH.sub.3).sub.2                                                               6-NO.sub.2                                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  3-Br   H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  6-Cl   CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  H      H  OC.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  3-F    H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Br        H      H  OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 S)                               Br        H      H  OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                            CO.sub.2 C.sub.2 H.sub.5                                                                 H      H  OCH.sub.3                                                                          CH(CH.sub.3)SC.sub.2 H.sub.5                           Br        H      H  OCH.sub.3                                                                          CH(CH.sub.2 CH.sub.3)SCH.sub.3                         SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          C(CH.sub.3)(SCH.sub.2 CH.sub.2 S)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(SCH.sub.3).sub.2                                    Br        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OCONHCH.sub.3                                 CF.sub.3  H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CF.sub.3  H      H  OCH.sub.3                                                                          CH.sub.2 SEt                                           SO.sub.2 N(Et).sub.2                                                                     H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCH.sub.2 CH.sub.3                                                                       H      H  OC.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                               O -n-C.sub.4 H.sub.9                                                                     H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               O .sub.-i-C.sub.3 H.sub.7                                                                H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               O CH.sub.2 CHCH.sub.2                                                                    H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CF.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CF.sub.3                                                                        5-CF.sub.3                                                                            H  OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 CF.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCF.sub.2 CF.sub.2 H                                                                     H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   OCF.sub.2 CF.sub.2 H                                                                     H      H  OC.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                   OCF.sub.2 CF.sub.2 H                                                                     H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   OSO.sub.2 C.sub.2 H.sub.5                                                                H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   CH.sub.2 OEt                                                                             6-F    H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H      H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            SO.sub.2 N(CH.sub.3)Et                                                                   H      H  OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 Et                                  SO.sub.2 N(CH.sub.3 )Et                                                                  H      H  OCH.sub.3                                                                          CH.sub.2 OCON(CH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3)Et                                                                   H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         149-152°                            CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         146-149°                            CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         146-149°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         136-146° d                          NO.sub.2  H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         152-156° d                          SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         185-188°                            Cl        H      H  OCH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.3                                                                 158-158.5°                          CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.3                                                                 58° d                               Cl        H      H  OCH.sub.3                                                                          CH(CH.sub.3)(S(O)CH.sub.3)                             CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(CH.sub.3)(SO.sub.2 CH.sub.3)                        CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                  SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.2 CH.sub.3                         NO.sub.2  6-Cl   H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                  SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                  Cl        H      H  OCH.sub.3                                                                          CH(CH.sub.3)(S(O)CH.sub.2 CH.sub.3)                    __________________________________________________________________________

                  TABLE 1i                                                         ______________________________________                                          ##STR43##                                                                                                    m.p.                                            R.sub.7     R.sub.8 R.sub.21                                                                              X   Y (°C.)                                  ______________________________________                                         Cl          H       H      Cl  CH(OCH.sub.3).sub.2  164-                                                      166°                                     CO.sub.2 CH.sub.3                                                                          H       H      Cl  CH(OCH.sub.3).sub.2 149-                                                       152°                                     SO.sub.2 CH.sub.3                                                                          H       H      Cl  CH(OCH.sub.3).sub.2                             NO.sub.2    H       H      Cl  CH(OC.sub.2 H.sub.5).sub.2                      CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H      Cl  CH.sub.2 SCH.sub.3                              CO.sub.2 C.sub.2 H.sub.5                                                                   H       CH.sub.3                                                                              Cl  CH.sub.2 SC.sub.2 H.sub.5                       CF.sub.3    H       H      Cl  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)               Br          H       H      Cl  CH(OCH.sub.3).sub.2                             CH.sub.3    H       H      Cl  CH(OCH.sub.3).sub.2                             C.sub.2 H.sub.5                                                                            H       H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      Cl  CH(OCH.sub.3).sub.2                             OCH.sub.3   H       CH.sub.3                                                                              Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       H      Cl  CH(OCH.sub.3).sub.2                             OCF.sub.2 CF.sub.2 H                                                                       H       H      Cl  CH(OCH.sub.3).sub.2                             CH.sub.2 OCH.sub.3                                                                         H       H      Cl  CH(OCH.sub.3).sub.2                             OSO.sub.2 CHCl.sub.2                                                                       H       H      Cl  CH(OCH.sub.3).sub.2                             SC.sub.2 H.sub.5                                                                           H       H      Cl  CH(OCH.sub.3).sub.2                             OSO.sub.2 CH.sub.3                                                                         H       H      Cl  CH(OCH.sub.3).sub.2                             OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H      Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      Cl  CH(OCH.sub.3).sub.2                             NO.sub.2    5-CF.sub.3                                                                             H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 -n-C.sub.3 H.sub.7                                                                3-Cl    H      Cl  CH(OCH.sub.3).sub.2                             OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             H      Cl  CH(OCH.sub.3).sub.2                             I           H       H      Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.3                                                                          H       H      Cl  C(CH.sub.3)(OCH.sub.3).sub.2                    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H      Cl  CH(OCH.sub.3).sub.2                             Cl          5-Cl    H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 CH.sub.3                                                                          5-Cl    H      Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.3                                                                          4-F     H      Cl  CH(OCH.sub.3).sub.2                             ______________________________________                                    

                  TABLE 1j                                                         ______________________________________                                          ##STR44##                                                                                                               m.p.                                 R.sub.7     R.sub.8 R.sub.21                                                                              X      Y       (°C.)                         ______________________________________                                         Cl          H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.3                                                                          H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2 113-                                                       121°                                  SO.sub.2 CH.sub.3                                                                          H       H      CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                          NO.sub.2    H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 C.sub.2 H.sub.5                                                                   H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CF.sub.3    H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          Br          H       H      CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                          CH(CH.sub.3).sub. 2                                                                        H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          C.sub.2 H.sub.5                                                                            H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OCH.sub.2 CHCHCH.sub.3                                                                     H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OCF.sub.2 CF.sub.2 H                                                                       H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CH.sub.2 OCH.sub.3                                                                         H       H      CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                          OSO.sub.2 CHCl.sub.2                                                                       H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SC.sub.2 H.sub.5                                                                           H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OSO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          NO.sub.2    5-CF.sub.3                                                                             H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2  -n-C.sub.3 H.sub.7                                                               3-Cl    H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.2 CH.sub.3                                                                 H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          I           H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          Cl          5-Cl    H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                          5-Cl    H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.3                                                                          4-F     H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OCH.sub.2 CHCH.sub.2                                                                       H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CH(OCH.sub.3)CH.sub.3                                                                      H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 CF.sub.3                                                                          H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SCHF.sub.2  H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OCH.sub.2 CHCHCH.sub.3                                                                     H       H      CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          Cl          H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.3                                                                          H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.2 CH.sub.3                                                                 H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3 ).sub.2                         SO.sub.2 CH.sub.3                                                                          H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                                 H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CH(CH.sub.3).sub.2                                                                         H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          OCH.sub.3   H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SCH.sub.3   H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                           -n-C.sub.4 H.sub.9                                                                        H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          O -n-C.sub.4 H.sub.9                                                                       H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          NO.sub.2    H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 -n-C.sub.4 H.sub.9                                                                H       CH.sub.3                                                                              CH.sub.3                                                                              CH(OCH.sub.3).sub.2                          Cl          H       H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 CH.sub.2 OCH.sub.3                                                                         H       H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 OCH.sub.3   H       H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3 ).sub.2                SC.sub.2 H.sub.5                                                                           H       H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 CO.sub.2 C.sub.2 H.sub.5                                                                   H       H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 CO.sub.2 CH.sub.3                                                                          5-Cl    H      CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 Cl          H       H      CH.sub.3                                                                              CH(SCH.sub.3).sub.2                          CO.sub.2 CH.sub.3                                                                          H       H      CH.sub.3                                                                              CH(SCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                          H       H      CH.sub.3                                                                              CH(SCH.sub.3).sub.2                          NO.sub.2    H       H      CH.sub.3                                                                              CH(SCH.sub.3).sub.2                          ______________________________________                                    

                  TABLE 1k                                                         ______________________________________                                          ##STR45##                                                                                                              m.p.                                  R.sub.7     R.sub.8                                                                               R.sub.21                                                                              X      Y       (°C.)                          ______________________________________                                         NO.sub.2    H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 Br          H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 Cl          H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 F           H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 SO.sub.2 CH.sub.3                                                                          H      CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                 H           H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 CO.sub.2 CH.sub.3                                                                          H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.3    H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                                 H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                                H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 OCH.sub.3   H      H      CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                 O -n-C.sub.3 H.sub.7                                                                       H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.2 OCH.sub.3                                                                         H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H      H      CH.sub.3                                                                              CH.sub.2 OTHP                                 ______________________________________                                    

                  TABLE 1l                                                         ______________________________________                                          ##STR46##                                                                                                               m.p.                                 R.sub.7     R.sub.8 R.sub.21                                                                               X      Y      (°C.)                         ______________________________________                                         Cl          H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.3                                                                          H       CH.sub.3                                                                               CH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                          H       H       CH.sub.3                                                                              CH.sub.2 OH                                 NO.sub.2    H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 C.sub.2 H.sub.5                                                                   H       H       CH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 CF.sub.3    H       H       CH.sub.3                                                                              CH.sub.2 OH                                 Br          H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CH.sub.3    H       H       CH.sub.3                                                                              CH.sub.2 OH                                 C.sub. 2 H.sub.5                                                                           H       H       CH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H       CH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H       CH.sub.3                                                                              CH.sub.2 OH                                 OCH.sub.3   H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       CH.sub.3                                                                               CH.sub.3                                                                              CH.sub.2 OH                                 OCF.sub.2 CF.sub.2 H                                                                       H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CH.sub.2 OCH.sub.3                                                                         H       H       CH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 CHCl.sub.2                                                                       H       H       CH.sub.3                                                                              CH.sub.2 OH                                 SC.sub.2 H.sub.5                                                                           H       H       CH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 CH.sub.3                                                                         H       H       CH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H       CH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H       CH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 C.sub.2 H.sub.5                                                                   H       H       CH.sub.3                                                                              CH.sub.2 OH                                 NO.sub.2    5-CF.sub.3                                                                             H       CH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                                3-Cl    H       CH.sub.3                                                                              CH.sub.2 OH                                 OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             H       CH.sub.3                                                                              CH.sub. 2 OH                                SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H       CH.sub.3                                                                              CH.sub.2 OH                                 Cl          5-Cl    H       CH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                          5-Cl    H       CH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.3                                                                          4-F     H       CH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 1m                                     __________________________________________________________________________      ##STR47##                                                                     R.sub.7    R.sub.8                                                                             R.sub.21                                                                           X     Y            m.p. (°C.)                       __________________________________________________________________________     NO.sub.2   H    H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                           NO.sub.2   H    CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                 NO.sub.2   H    H   CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                   Br         H    H   CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                               Cl         H    H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                          F          H    H   CH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                            F          H    H   CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                             SO.sub.2 CH.sub.3                                                                         H    H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOC.sub.2 H.sub.5                          SO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                          SO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                    SO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH.sub.2 SCH.sub.2 CH.sub.3                          H          H    H   CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                 CO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3).sub.2                        CO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                             CO.sub.2 CH.sub.3                                                                         H    CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                 CO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                            CH.sub.3   H    H   CH.sub.2 CH.sub.3                                                                    CH(OC.sub.2 H.sub.5).sub.2                           CH.sub.3   H    H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                   SO.sub.2 N(CH.sub.3).sub.2                                                                H    H   CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                 SO.sub.2 N(CH.sub.3).sub.2                                                                H    H   CH.sub.3                                                                             CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H    H   CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7                    SO.sub.2 -n-C.sub.3 H.sub.7                                                               H    H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                           OCH.sub.3  H    H   CH.sub.3                                                                             CH(SCH.sub.2 CH.sub.2 S)                             OCH.sub.3  H    H   CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                   O -n-C.sub.3 H.sub.7                                                                      H    H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                          Cl         H    H   CH.sub.3                                                                             C(CH.sub.3)(SCH.sub.3).sub.2                         CO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH(C.sub.2 H.sub.5)SCH.sub.3                         SO.sub.2 N(CH.sub.3).sub.2                                                                H    H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                    I          H    H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)           Br         H    CH.sub.3                                                                           OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                               CF.sub.3   H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             CF.sub.3   H    H   OCH.sub.3                                                                            CH.sub.2 SEt                                         SO.sub.2 N(Et).sub.2                                                                      H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             OCH.sub.2 CH.sub.3                                                                        H    H   OC.sub.2 H.sub.5                                                                     CH(OCH.sub.2 CH.sub.2 O)                             O -n-C.sub.4 H.sub.9                                                                      H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             O .sub.-i-C.sub.3 H.sub.7                                                                 H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             OCH.sub.2 CHCH.sub.2                                                                      H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             SO.sub.2 CF.sub.3                                                                         H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             SO.sub.2 CF.sub.3                                                                         5-CF.sub.3                                                                          H   OCH.sub.3                                                                            CH(OEt).sub.2                                        SO.sub.2 CF.sub.3                                                                         H    H   OCH.sub.3                                                                            CH(OEt).sub.2                                        SO.sub.2 -n-C.sub.3 H.sub.7                                                               H    H   OCH.sub.3                                                                            CH(OEt).sub.2                                        SO.sub.2 -n-C.sub.3 H.sub.7                                                               H    CH.sub.3                                                                           OCH.sub.3                                                                            CH(OEt).sub.2                                        SO.sub.2 -n-C.sub.3 H.sub.7                                                               H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                             OCF.sub.2 CF.sub.2 H                                                                      H    H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                 OCF.sub.2 CF.sub.2 H                                                                      H    H   OC.sub.2 H.sub.5                                                                     CH.sub.2 OCOCH.sub.3                                 OCF.sub.2 CF.sub.2 H                                                                      H    H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                 OSO.sub.2 C.sub.2 H.sub.5                                                                 H    H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                 CH.sub.2 OEt                                                                              6-F  H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                 CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                             H    H   OCH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2 O)                          SO.sub.2 N(CH.sub.3)Et                                                                    H    H   OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 Et                                SO.sub.2 N(CH.sub.3)Et                                                                    H    H   OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                        SO.sub.2 N(CH.sub.3)Et                                                                    H    H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                    Cl         H    H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                   CO.sub.2 CH.sub.3                                                                         H    H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                   CO.sub.2 CH.sub.2 CH.sub.3                                                                H    H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                   SO.sub.2 N(CH.sub.3).sub.2                                                                H    H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                   NO.sub.2   H    H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                   SO.sub.2 CH.sub.3                                                                         H    H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                   Cl         H    H   OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                           CO.sub.2 CH.sub.3                                                                         H    H   OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                           O -n-C.sub.3 H.sub.7                                                                      H    H   CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                 CH.sub.2 OCH.sub.3                                                                        H    H   CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                 CH.sub.2 OCH.sub.3                                                                        H    H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                          CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H    H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                           SO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                                Cl         H    H   CH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                                CO.sub.2 CH.sub.3                                                                         H    H   CH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                                OCH.sub.3  H    H   OCH.sub.3                                                                            CH(CH.sub.3)(S(O)CH.sub.3)                           CH.sub.2 OCH.sub.3                                                                        H    H   OCH.sub.3                                                                            CH(CH.sub.3)(S(O)CH.sub.3)                           __________________________________________________________________________

                  TABLE 1n                                                         ______________________________________                                          ##STR48##                                                                                                             m.p.                                   R.sub.7     R.sub.8 R.sub.21  X Y       (°C.)                           ______________________________________                                         Cl          H       H OCH.sub.3 CH(OCH.sub.3).sub.2 117-                                                       121°                                    CO.sub.2 CH.sub.3                                                                          H       HOCH.sub.3  CH(OCH.sub.3).sub.2 135-                                                       158°                                    SO.sub.2 CH.sub.3                                                                          H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            NO.sub.2    H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            CO.sub.2 CH(CH.sub.3).sub.2                                                                H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            CO.sub.2 C.sub.2 H.sub.5                                                                   H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            CF.sub.3    H       HOCH.sub.2 CH.sub.3                                                                        CH(OCH.sub.3).sub.2                            Br          H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            CH.sub.3    H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            C.sub.2 H.sub.5                                                                            H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3).sub.2                                                                 H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            OCH.sub.3   H       HOCH.sub.2 CH.sub.3                                                                        CH(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       CH.sub.3 OCH.sub.3                                                                         CH(OCH.sub.3).sub.2                            OCF.sub.2 CF.sub.2 H                                                                       H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            CH.sub.2 OCH.sub.3                                                                         H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            OSO.sub.2 CHCl.sub.2                                                                       H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            SC.sub.2 H.sub.5                                                                           H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            OSO.sub.2 CH.sub.3                                                                         H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            OSO.sub.2 C.sub.2 H.sub.5                                                                  H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 C.sub.2 H.sub.5                                                                   H       HOCH.sub.3  CH(OCH.sub.3).sub.2                            NO.sub.2    5-CF.sub.3                                                                             HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2  -n-C.sub.3 H.sub.7                                                               3-Cl    HOCH.sub.3  CH(OCH.sub.3).sub.2                            OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             HOCH.sub.3  CH(OCH.sub.3).sub.2                            CH.sub.2 CH.sub.3                                                                          H       HOCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                   CO.sub.2 CH.sub.3                                                                          H       HOCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                   CH.sub.2 Cl H       HOCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                   SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             HOCH.sub.3  CH(OCH.sub.3).sub.2                            Cl          5-Cl    HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                          5-Cl    HOCH.sub.3  CH(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                          4-F     HOCH.sub.3  CH(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.2 CH.sub.3                                                                 H       HOCH.sub.3  C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2            I           H       HOCH.sub.3  C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2            Cl          H       HOCH.sub.3  C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2            ______________________________________                                    

                  TABLE 1o                                                         ______________________________________                                          ##STR49##                                                                                                           m.p.                                     R.sub.7     R.sub.8                                                                              R.sub.21 X  Y       (°C.)                             ______________________________________                                         NO.sub.2    H     HOCH.sub.3  CH.sub.2 OTHP                                    Br          H     HOCH.sub.3  CH.sub.2 OTHP                                    Cl          H     HOCH.sub.3  CH.sub.2 OTHP                                                                          136-139°                          SO.sub.2 CH.sub.3                                                                          H     HOCH.sub.3  CH.sub.2 OTHP                                    F           H     HOCH.sub.3  CH.sub.2 OTHP                                    H           H     HOCH.sub.3  CH.sub.2 OTHP                                    CO.sub.2 CH.sub.3                                                                          H     HOCH.sub.3  CH.sub.2 OTHP                                    CH.sub.3    H     HOCH.sub.3  CH.sub.2 OTHP                                    SO.sub.2 N(CH.sub.3).sub.2                                                                 H     HOCH.sub.3  CH.sub.2 OTHP                                    SO.sub.2 -n-C.sub.3 H.sub. 7                                                               H     HOCH.sub.3  CH.sub.2 OTHP                                    OCH.sub.3   H     CH.sub.3 OCH.sub.3                                                                         CH.sub.2 OTHP                                    O -n-C.sub.3 H.sub.7                                                                       H     HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                    CH.sub.2 OCH.sub.3                                                                         H     HOCH.sub.3  CH.sub.2 OTHP                                    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H     HOCH.sub.3  CH.sub.2 OTHP                                    I           H     HOCH.sub.3  CH.sub.2 OTHP                                    CH.sub.2 Cl H     HOCH.sub.3  CH.sub.2 OTHP                                    ______________________________________                                    

                  TABLE 1p                                                         ______________________________________                                          ##STR50##                                                                                                         m.p.                                       R.sub.7     R.sub.8 R.sub.21                                                                         XY            (°C.)                               ______________________________________                                         Cl          HH        OCH.sub.3 CH.sub.2 OH                                                                        133-135°                            CO.sub.2 CH.sub.3                                                                          HH        OCH.sub.3 CH.sub.2 OH                                                                        115°d                               SO.sub.2 CH.sub.3                                                                          HH        OCH.sub.3 CH.sub.2 OH                                    NO.sub.2    HH        OCH.sub.3 CH.sub.2 OH                                    CO.sub.2 CH(CH.sub.3).sub.2                                                                HH        OCH.sub.3 CH.sub.2 OH                                    CO.sub.2 C.sub.2 H.sub.5                                                                   HH        OCH.sub.3 CH.sub.2 OH                                    CF.sub.3    HH        OCH.sub.3 CH.sub.2 OH                                    Br          HH        OCH.sub.2 CH.sub.3 CH.sub.2 OH                           CH.sub.3    HH        OCH.sub.3 CH.sub.2 OH                                    C.sub.2 H.sub.5                                                                            HH        OCH.sub.3 CH.sub.2 OH                                    SO.sub.2 -n-C.sub.3 H.sub.7                                                                HH        OCH.sub.3 CH.sub.2 OH                                                                        152°d                               SO.sub.2 N(CH.sub.3).sub.2                                                                 HH        OCH.sub.3 CH.sub.2 OH                                    OCH.sub.3   HH        OCH.sub.3 CH.sub.2 OH                                    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               HH        OCH.sub.3 CH.sub.2 OH                                    OCF.sub.2 CF.sub.2 H                                                                       HH        OCH.sub.3 CH.sub.2 OH                                    CH.sub.2 OCH.sub.3                                                                         HH        OCH.sub.3 CH.sub.2 OH                                    OSO.sub.2 CHCl.sub.2                                                                       HH        OCH.sub.3 CH.sub.2 OH                                    SC.sub.2 H.sub.5                                                                           HCH.sub.3 OCH.sub.3 CH.sub.2 OH                                    OSO.sub.2 CH.sub.3                                                                         HH        OCH.sub.3 CH.sub.2 OH                                    OSO.sub.2 C.sub.2 H.sub.5                                                                  HH        OCH.sub.3 CH.sub.2 OH                                    CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       HH        OCH.sub.3 CH.sub.2 OH                                    SO.sub.2 C.sub.2 H.sub.5                                                                   HH        OCH.sub.3 CH.sub.2 OH                                    NO.sub.2    5-CF.sub.3 H                                                                             OCH.sub.2 CH.sub.3 CH.sub.2 OH                           SO.sub.2 -n-C.sub. 3 H.sub.7                                                               3-ClH     OCH.sub.3 CH.sub.2 OH                                    OC.sub.2 H.sub.5                                                                           5-NO.sub.2 H                                                                             OCH.sub.3 CH.sub.2 OH                                    I           HH        OCH.sub.3 CH.sub.2 OH                                    CH.sub.2 Cl HH        OCH.sub.3 CH.sub.2 OH                                    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2 H                                                                             OCH.sub.3 CH.sub.2 OH                                    Cl          5-ClH     OCH.sub.3 CH.sub.2 OH                                    SO.sub.2 CH.sub.3                                                                          5-ClH     OCH.sub.3 CH.sub.2 OH                                    CO.sub.2 CH.sub.3                                                                          4-FH      OCH.sub.3 CH.sub.2 OH                                    ______________________________________                                    

                  TABLE 1q                                                         ______________________________________                                          ##STR51##                                                                     R.sub.7     R.sub.8                                                                              R.sub.21                                                                              X       Y     m.p. (°C.)                       ______________________________________                                         NO.sub.2    H     H      OCH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                    NO.sub.2    H     H      OCH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                          NO.sub.2    H     H      OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                            Br          H     H      OCH.sub.3                                                                              CH.sub.2 OCONHCH.sub.3                        Cl          H     H      OCH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                   F           H     H      OCH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                     F           H     H      OCH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                      SO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                   SO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub. 2 O)                   SO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)              SO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 SCH.sub.3                            H           H     H      OCH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                          CO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                 CO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                      CO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                          CO.sub.2 CH.sub.3                                                                          H     CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                     CH.sub.3    H     H      OCH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                    CH.sub.3    H     H      OCH.sub.3                                                                              CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5            SO.sub.2 N(CH.sub.3).sub.2                                                                 H     H      OCH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2          SO.sub.2 N(CH.sub.3).sub.2                                                                 H     H      OCH.sub.3                                                                              CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7          SO.sub.2 -n-C.sub.3 H.sub.7                                                                H     H      OCH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7              SO.sub.2 -n-C.sub.3 H.sub.7                                                                H     H      OCH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                    OCH.sub.3   H     H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.2 CH.sub.2 O)                      OCH.sub.3   H     H      OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                            O -n-C.sub.3 H.sub.7                                                                       H     H      OCH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                   NO.sub.2    H     H      OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                    SO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                    CO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H     H      OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                    O -n-C.sub.3 H.sub.7                                                                       H     H      OCH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2          CH.sub.2 OCH.sub.3                                                                         H     H      OCH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                          CH.sub.2 OCH.sub.3                                                                         H     H      OCH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                   CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H     H      OCH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                    I           H     H      OCH.sub.3                                                                              CH(CH.sub.3)SCH.sub.3                         CH.sub.2 Cl H     H      OCH.sub.3                                                                              CH(C.sub.2 H.sub.5)SO.sub.2 CH.sub.3          CO.sub.2 CH.sub.2 CH.sub.3                                                                 H     H      OCH.sub.3                                                                              C(CH.sub.3)(SCH.sub.2 CH.sub.2 S)             NO.sub.2    H     H      OCH.sub.3                                                                              C(C.sub.2 H.sub.5)(SCH.sub.3).sub.2           SO.sub.2 N(CH.sub. 3).sub.2                                                                H     H      OCH.sub.3                                                                              CH(SC.sub.2 H.sub.5).sub.2                    OCHF.sub.2  H     H      OCH.sub.3                                                                              CH(SCH.sub.3).sub.2                           Cl          H     H      OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3           Br          H     H      OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                    CH.sub.2 OCH.sub.3                                                                         H     H      OCH.sub.3                                                                              C(CH.sub.3)(SCH.sub.3).sub.2                  SO.sub.2 N(CH.sub.3).sub.2                                                                 H     H      OCH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                         NO.sub.2    H     H      OCH.sub.3                                                                              CH.sub.2 S(O)CH.sub.2 CH.sub.3                CH.sub.2 OCH.sub.3                                                                         H     H      OCH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                         SO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH(CH.sub.3)(S(O)CH.sub.3)                    CO.sub.2 CH.sub.3                                                                          H     H      OCH.sub.3                                                                              CH(CH.sub.3)(S(O)CH.sub.3)                    ______________________________________                                    

                  TABLE 1r                                                         ______________________________________                                          ##STR52##                                                                                                         m.p.                                       R.sub.7  R.sub.8 X  Y               Z(°C.)                              ______________________________________                                         H        HCH.sub.3  CH(OCH.sub.3).sub.2                                                                            CH                                         H        HOCH.sub.3 CH.sub.2 SCH.sub.3                                                                             CH                                         Cl       HCH.sub.3  CH.sub.2 SO.sub.2 CH.sub.3                                                                     CH                                         Cl       HOCH.sub.3 C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                                                              CH                                         Cl       HCH.sub.3  CH(OCH.sub.3).sub.2                                                                            CH                                         Cl       5-ClOCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                            N                                          NO.sub.2 HCH.sub.3  CH(OCH.sub.3).sub.2                                                                            N                                          NO.sub.2 HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                            CH                                         CO.sub.2 CH.sub.3                                                                       HCH.sub.3  CH(OCH.sub.3).sub.2                                                                            CH                                         CO.sub.2 CH.sub.3                                                                       HOCH.sub.3 CH(OEt).sub.2   CH                                         CO.sub.2 CH.sub.3                                                                       HOC.sub.2 H.sub.5                                                                         CH(OEt).sub.2   CH                                         CO.sub.2 CH.sub.2 CH.sub.3                                                              HCH.sub.3  CH.sub. 2 OTHP  N                                          CO.sub.2 CH.sub.2 CH.sub.3                                                              HC.sub.2 H.sub.5                                                                          CH.sub.2 OH     N                                          CO.sub.2 CH.sub.2 CH.sub.3                                                              HCl        CH.sub.2 SCH.sub.3                                                                             N                                          SO.sub.2 CH.sub.3                                                                       HCH.sub.3  CH(CH.sub.3)SC.sub.2 H.sub.5                                                                   CH                                         SO.sub.2 CH.sub.3                                                                       HOC.sub.2 H.sub.5                                                                         CH(CH.sub.3)SC.sub.2 H.sub.5                                                                   CH                                         SO.sub.2 CH.sub.3                                                                       HCH.sub.3  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                              CH                                         SC.sub.2 H.sub.5                                                                        HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                              N                                          SC.sub.2 H.sub.5                                                                        HCH.sub.3  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                              N                                          SC.sub.2 H.sub.5                                                                        HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                            CH                                         SO.sub.2 N(CH.sub.3).sub.2                                                              HC.sub.2 H.sub.5                                                                          CH(OCH.sub.3).sub.2                                                                            CH                                         SO.sub.2 N(CH.sub.3).sub.2                                                              3-CH.sub.3 OCH.sub.3                                                                      CH(OCH.sub.3).sub.2                                                                            CH                                         SO.sub.2 N(CH.sub.3).sub.2                                                              HCH.sub.3  CH(OCH.sub.3).sub.2                                                                            CH                                         C.sub.2 H.sub.5                                                                         HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                            CH                                         C.sub.2 H.sub.5                                                                         HCH.sub.3  CH(CH.sub.3)SO.sub.2 CH.sub.3                                                                  N                                          C.sub.2 H.sub.5                                                                         HOCH.sub.3 CH(CH.sub.3)SO.sub. 2 CH.sub.3                                                                 N                                          C.sub.2 H.sub.5                                                                         HOCH.sub.3 CH(CH.sub.3)SO.sub.2 CH.sub.3                                                                  CH                                         O .sub.-i-C.sub.3 H.sub.7                                                               HCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                                                                       CH                                         O .sub.-i-C.sub.3 H.sub.7                                                               HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                       CH                                         F        HCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                                                                       CH                                         Br       HOCH.sub.3 CH(OCH(CH.sub.3)CH.sub.2 O)                                                                    N                                          CH.sub.2 OCH.sub.3                                                                      HCH.sub.3  CH(SCH.sub.2 CH.sub.2 S)                                                                       CH                                         CH.sub.2 OCH.sub.3                                                                      HOCH.sub.3 CH(SCH.sub.3).sub.2                                                                            CH                                         CH.sub.2 OCH.sub.3                                                                      6-ClOCH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                                                                     CH                                         SO.sub.2 -n-C.sub.3 H.sub.7                                                             HCH.sub.3  CH(CH.sub.3)SCH.sub.3                                                                          CH                                         CO.sub.2 CH.sub.3                                                                       HOCH.sub.3 CH.sub.2 S(O)CH.sub.3                                                                          CH                                         CO.sub.2 CH.sub.3                                                                       HOCH.sub.3 CH.sub.2 S(O)CH.sub.3                                                                          N                                          ______________________________________                                    

                  TABLE 2a                                                         ______________________________________                                          ##STR53##                                                                                                           m.p.                                     R.sub.14 R.sub.15 R.sub.21 X                                                                            Y            (°C.)                             ______________________________________                                         Cl       HHCH.sub.3      CH(OCH.sub.3).sub.2                                   Br       HHCH.sub.3      CH(OCH.sub.3).sub.2                                   F        HHOCH.sub.3     CH(OCH.sub.3).sub.2                                   H        HHOCH.sub.3     CH(OCH.sub.3).sub.2                                   Cl       HHCl            CH(OCH.sub.3).sub.2                                   Cl       3-ClHCH.sub.3   CH(OCH.sub.3).sub.2                                   Cl       HHOCH.sub.3     CH(OCH.sub.3).sub.2                                   OCH.sub.3                                                                               HHCH.sub.3      CH(OCH.sub.3).sub.2                                   CH.sub.3 HHOCH.sub.2 CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                   Br       HHCl            CH(OCH.sub.3).sub.2                                   CH.sub.3 H HCH.sub.3     CH(OCH.sub.3).sub.2                                   NO.sub.2 HCH.sub.3 OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   CH.sub.3 4-FHOCH.sub.3   CH(OCH.sub.3).sub.2                                   Cl       6-NO.sub.2 HOCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                   NO.sub.2 HHCH.sub.3      CH(OCH.sub.3).sub.2                                   NO.sub.2 HHCl            CH(OCH.sub.3).sub.2                                   Cl       6-FHCH.sub.2 CH.sub.3                                                                          CH(OCH.sub.3).sub.2                                   NO.sub.2 4-ClHCH.sub.3   CH(OCH.sub.3).sub.2                                   Cl       5-OCH.sub.3 HOCH.sub.3                                                                         CH(OCH.sub.3).sub.2                                   F        HHCH.sub.3      CH(OCH.sub.3).sub.2                                   H        HHCH.sub.3      CH(OCH.sub.3).sub.2                                   SO.sub.2 N(CH.sub.3).sub.2                                                              HHOCH.sub.3     CH(OCH.sub.3).sub.2                                   SO.sub.2 N(CH.sub.3).sub.2                                                              HHOCH.sub.2 CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                   OCH.sub.3                                                                               HCH.sub.3 CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   OSO.sub.2 CH.sub.3                                                                      HHCH.sub.3      CH(OCH.sub.3).sub.2                                   Cl       HHCH.sub.3      C(CH.sub.3)(OCH.sub.3).sub.2                          Br       HHCH.sub.3      C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                   OCH.sub.3                                                                               HHCH.sub.3      C(CH.sub.3)(OCH.sub.3).sub.2                          NO.sub. 2                                                                               HHCH.sub.3      C(CH.sub.3)(OCH.sub.3).sub.2                          ______________________________________                                    

                  TABLE 2b                                                         ______________________________________                                          ##STR54##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                              X       Y        (°C.)                         ______________________________________                                         Cl       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Br       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 F        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 H        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 Cl       3-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                 OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 CH.sub.3 H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.3 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 NO.sub.2 H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.3 4-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 NO.sub.2 H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                 Cl       6-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                                 NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 F        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 H        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 ______________________________________                                    

                  TABLE 2c                                                         ______________________________________                                          ##STR55##                                                                                                               m.p.                                 R.sub.14  R.sub.15 R.sub.21                                                                              X        Y      (°C.)                         ______________________________________                                         Cl        H        H      CH.sub.3 CH.sub.2 OH                                 Br        H        H      CH.sub.3 CH.sub.2 OH                                 F         H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 H         H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 Cl        3-Cl     H      CH.sub.3 CH.sub.2 OH                                 Cl        H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 OCH.sub.3 H        H      CH.sub.2 CH.sub.3                                                                       CH.sub.2 OH                                 CH.sub.3  H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 CH.sub.3  H        H      CH.sub.3 CH.sub.2 OH                                 NO.sub.2  H        CH.sub.3                                                                              OCH.sub.3                                                                               CH.sub.2 OH                                 CH.sub.3  4-F      H      OCH.sub.3                                                                               CH.sub.2 OH                                 Cl        6-NO.sub. 2                                                                             H      OCH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 NO.sub.2  H        H      CH.sub.3 CH.sub.2 OH                                 Cl        6-F      H      CH.sub.3 CH.sub.2 OH                                 NO.sub.2  4-Cl     H      CH.sub.3 CH.sub.2 OH                                 Cl        5-OCH.sub.3                                                                             H      OCH.sub.3                                                                               CH.sub.2 OH                                 F         H        H      CH.sub.3 CH.sub.2 OH                                 H         H        H      CH.sub.3 CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 OCH.sub.3 H        H      CH.sub.3 CH.sub.2 OH                                 OSO.sub.2 CH.sub.3                                                                       H        CH.sub.3                                                                              CH.sub.3 CH.sub.2 OH                                 SO.sub.2 .sub.-n-C.sub.3 H.sub.7                                                         H        H      OCH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 ______________________________________                                    

                  TABLE 2d                                                         ______________________________________                                          ##STR56##                                                                     R.sub.14 R.sub.15                                                                               R.sub.21                                                                              X     Y        m.p. (°C.)                       ______________________________________                                         Cl       H       H      CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                         Br       H       H      CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                             F        H       H      OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                        H        H       H      OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                      Cl       3-Cl    H      CH.sub.3                                                                             CH.sub.2 SCH.sub.3                               Cl       H       H      OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                       OCH.sub.3                                                                               H       H      CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                CH.sub.3 H       H      OCH.sub.3                                                                            CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7             CH.sub.3 H       H      CH.sub.3                                                                             CH.sub.2 OCO.sub. 2 C.sub.2 H.sub.5              NO.sub.2 H       H      OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                       CH.sub.3 4-F     CH.sub.3                                                                              OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                         Cl       6-NO.sub.2                                                                             H      OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                             NO.sub.2 H       H      CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                      Cl       6-F     H      CH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7            NO.sub.2 4-Cl    H      CH.sub.3                                                                             CH.sub.2 SCH.sub.3                               Cl       5-OCH.sub.3                                                                             H     OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                        F        H        H     CH.sub.3                                                                             CH(SCH(CH.sub.3)CH.sub.2 S)                      H        H        H     CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                       SO.sub.2 N(CH.sub.3).sub.2                                                              H        H     OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                         SO.sub.2 N(CH.sub.3).sub.2                                                              H        H     OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                           OCH.sub.3                                                                               H        H     CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7                OSO.sub.2 CH.sub.3                                                                      H        H     CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                             SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H     OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                       Cl       H        H     OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                              NO.sub.2 H        H     OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3              OSO.sub.2 CH.sub.3                                                                      H        H     OCH.sub.3                                                                            CH(CH.sub.3)SCH.sub.3                            CH.sub.3 H        H     OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                       SO.sub.2 CH.sub.3                                                                       H        H     OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.2 CH.sub.2 CH.sub.2          ______________________________________                                                                       S)                                          

                  TABLE 2e                                                         ______________________________________                                          ##STR57##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                              X       Y        (°C.)                         ______________________________________                                         Cl       H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Br       H        H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           F        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           Cl       3-Cl     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           CH.sub.3 H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           CH.sub.3 H        CH.sub.3                                                                              CH.sub.3                                                                               CH(OCH.sub.3).sub. 2                          NO.sub.2 H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           CH.sub.3 4-F      H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           NO.sub.2 H        H      CH.sub.2                                                                               CH(OCH.sub.3).sub.2                           Cl       6-F      H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           NO.sub.2 4-Cl     H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           F        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  Cl       H        H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  F        H        H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  SO.sub.2 CH.sub.2 CH.sub.3                                                              H        H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  NO.sub.2 H        H      OCH.sub.3                                                                              C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2         ______________________________________                                    

                  TABLE 2f                                                         ______________________________________                                          ##STR58##                                                                                                              m.p.                                  R.sub.14 R.sub.15 R.sub.21                                                                              X       Y       (°C.)                          ______________________________________                                         Cl       H        CH.sub.3                                                                              CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                 Br       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 F        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 H        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 Cl       3-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                 OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 CH.sub.3 H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.3 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 NO.sub.2 H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.3 4-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 NO.sub.2 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       6-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                                 NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 F        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 H        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 OCH.sub.3                                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                 OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 ______________________________________                                    

                  TABLE 2g                                                         ______________________________________                                          ##STR59##                                                                                                              m.p.                                  R.sub.14 R.sub.15 R.sub.21                                                                               X       Y      (°C.)                          ______________________________________                                         Cl       H        H       CH.sub.3                                                                               CH.sub.2 OH                                  Br       H        H       CH.sub.3                                                                               CH.sub.2 OH                                  F        H        H       OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                  H        H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  Cl       3-Cl     H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OH                                  CH.sub.3 H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  CH.sub.3 H        H       CH.sub.3                                                                               CH.sub.2 OH                                  NO.sub.2 H        H       OCH.sub.3                                                                              CH.sub. 2 OH                                 CH.sub.3 4-F      H       OCH.sub.3                                                                              CH.sub.2 OH                                  Cl       6-NO.sub.2                                                                              H       OCH.sub.3                                                                              CH.sub.2 OH                                  NO.sub.2 H        H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       6-F      H       CH.sub.3                                                                               CH.sub.2 OH                                  NO.sub.2 4-Cl     H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       5-OCH.sub.3                                                                             H       OCH.sub.3                                                                              CH.sub.2 OH                                  F        H        H       CH.sub.3                                                                               CH.sub.2 OH                                  H        H        H       CH.sub.3                                                                               CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                               OCH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                              H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OH                                  OSO.sub.2 CH.sub.3                                                                      H        H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  ______________________________________                                    

                  TABLE 2h                                                         ______________________________________                                          ##STR60##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                              X     Y          (°C.)                         ______________________________________                                         Cl       H        H      CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                        Br       H        H      CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                            F        H        H      OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                       H        H        H      OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                     Cl       3-Cl     H      CH.sub.3                                                                             CH.sub.2 SCH.sub.3                              Cl       H        H      OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                      OCH.sub.3                                                                               H        H      CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)               CH.sub.3 H        H      OCH.sub.3                                                                            CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7            CH.sub.3 H        H      CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5              NO.sub.2 H        H      OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                      CH.sub.3 4-F      H      OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                        Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                            NO.sub.2 H        CH.sub.3                                                                              CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                     Cl       6-F      H      CH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7           NO.sub.2 4-Cl     CH.sub.3                                                                              CH.sub.3                                                                             CH.sub.2 SCH.sub.3                              Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                       F        H        H      CH.sub.3                                                                             CH(SCH(CH.sub.3)CH.sub.2 S)                     H        H        H      CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                      SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                        SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                          OCH.sub.3                                                                               H        H      CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7               OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                            SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                      Cl       H        H      OCH.sub. 3                                                                           CH.sub.2 SO.sub.2 CH.sub.3                      H        H        H      OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                             OCH.sub.3                                                                               H        H      CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)               SO.sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                             CH(C.sub.2 H.sub.5)SO.sub.2 CH.sub.3            NO.sub.2 H        H      CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3             NO.sub.2 H        H      CH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                           ______________________________________                                    

                                      TABLE 3a                                     __________________________________________________________________________      ##STR61##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                           X     Y        m.p (°C.)                                __________________________________________________________________________     Cl     H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                     177-178° d                               Br     H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      F      H    H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H      H    H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      Cl     H    H   Cl    CH(OCH.sub.3).sub.2                                      Cl     3-Cl H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      Cl     H    H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     156-175°  d                              OCH.sub.3                                                                             H    H   CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                      CH.sub.3                                                                              H    H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      Br     H    H   Cl    CH(OCH.sub.3).sub.2                                      CH.sub.3                                                                              H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      NO.sub.2                                                                              H    H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      CH.sub.3                                                                              4-F  H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      Cl     6-NO.sub.2                                                                          H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      NO.sub.2                                                                              H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      NO.sub.2                                                                              H    H   Cl    CH(OCH.sub.3).sub.2                                      Cl     6-F  CH.sub.3                                                                           CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      NO.sub.2                                                                              4-Cl H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      Cl     5-OCH.sub.3                                                                         H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      F      H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H      H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 N(CH.sub.3).sub.2                                                            H    H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      SO.sub.2 N(CH.sub.3).sub.2                                                            H    H   OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                      OCH.sub.3                                                                             H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      OSO.sub.2 CH.sub.3                                                                    H    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      Cl     H    H   CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                             NO.sub.2                                                                              H    H   CH.sub.3                                                                             C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                      OCH.sub.3                                                                             H    H   CH.sub.3                                                                             C(C.sub.2 H.sub. 5)(OCH.sub.3).sub.2                     Br     H    H   OCH.sub.3                                                                            C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                      __________________________________________________________________________

                  TABLE 3b                                                         ______________________________________                                          ##STR62##                                                                                                               m.p.                                 R.sub.14   R.sub.15 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         Cl         H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               Br         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               F          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               Cl         3-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               OCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               CH.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CH.sub.3   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CH.sub.3   4-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                               Cl         6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                               NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         6-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   4-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                               F          H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               H          H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               OCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               OSO.sub.2 CH.sub.3                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               O -n-C.sub.3 H.sub.7                                                                      H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 3c                                                         ______________________________________                                          ##STR63##                                                                                                              m.p.                                  R.sub.14 R.sub.15 R.sub.21                                                                               X       Y      (°C.)                          ______________________________________                                         Cl       H        CH.sub.3                                                                               CH.sub.3                                                                               CH.sub.2 OH                                  Br       H        H       CH.sub.3                                                                               CH.sub.2 OH                                  F        H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  H        H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  Cl       3-Cl     H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OH                                  CH.sub.3 H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  CH.sub.3 H        H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                  NO.sub.2 H        H       OCH.sub.3                                                                              CH.sub.3 OH                                  CH.sub.3 4-F      H       OCH.sub.3                                                                              CH.sub.2 OH                                  Cl       6-NO.sub.2                                                                              H       OCH.sub.3                                                                              CH.sub.2 OH                                  NO.sub.2 H        H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       6-F      H       CH.sub.3                                                                               CH.sub.2 OH                                  NO.sub.2 4-Cl     H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       5-OCH.sub.3                                                                             H       OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                  F        H        H       CH.sub.3                                                                               CH.sub.2 OH                                  H        H        H       CH.sub.3                                                                               CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                               OCH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                              H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OH                                  OSO.sub.2 CH.sub.3                                                                      H        H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  ______________________________________                                    

                                      TABLE 3d                                     __________________________________________________________________________      ##STR64##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X     Y            m.p. (°C.)                            __________________________________________________________________________     Cl     H    H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                                                    180-182° d                            Br     H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      F      H    H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 H      H    CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               Cl     3-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                OCH.sub.3                                                                             H    H  CH.sub.2 CH.sub.3                                                                    CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                         CH.sub.3                                                                              H    H  OCH.sub.3                                                                            CH.sub.2 OCO .sub.-i-C.sub. 3 H.sub.7                     CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                        NO.sub.2                                                                              H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                CH.sub.3                                                                              4-F  H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      NO.sub.2                                                                              H    H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                               Cl     6-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7                     NO.sub.2                                                                              4-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 F      H    CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                               H      H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                                SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCONHCH.sub.3                                    OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7                         OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      SO.sub.2 -n-C.sub.3 H.sub.7                                                           H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub. 5).sub.2                               Cl     H    H  OCH.sub.3                                                                            CH(CH.sub.3)SCH.sub.3                                     Br     H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)                F      H    H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                       OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 S(O)CH.sub.2 CH.sub.3                            __________________________________________________________________________

                  TABLE 3e                                                         ______________________________________                                          ##STR65##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                              X       Y        (°C.)                         ______________________________________                                         Cl       H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Br       H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           F        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           Cl       3-Cl     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           CH.sub.3 H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           CH.sub.3 H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           NO.sub.2 H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           CH.sub.3 4-F      CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           NO.sub.2 H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       6-F      H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           F        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  Cl       H        H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  NO.sub.2 H        H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  OCH.sub.3                                                                               H        H      OCH.sub. 3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                  F        H        H      CH.sub.3                                                                               C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2         ______________________________________                                    

                  TABLE 3f                                                         ______________________________________                                          ##STR66##                                                                                                              m.p.                                  R.sub.14 R.sub.15 R.sub.21                                                                              X       Y       (°C.)                          ______________________________________                                         Cl       H        CH.sub.3                                                                              CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                 Br       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 F        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 H        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 Cl       3-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 CH.sub.3 H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 CH.sub.3 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 NO.sub.2 H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                 CH.sub. 3                                                                               4-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 NO.sub.2 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       6-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                                 NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                 Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 F        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 H        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                                 SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                 OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                 ______________________________________                                    

                  TABLE 3g                                                         ______________________________________                                          ##STR67##                                                                                                              m.p.                                  R.sub.14 R.sub.15 R.sub.21                                                                               X       Y      (°C.)                          ______________________________________                                         Cl       H        H       CH.sub.3                                                                               CH.sub.2 OH                                  Br       H        H       CH.sub.3                                                                               CH.sub.2 OH                                  F        H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  H        H        H       OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                  Cl       3-Cl     H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OH                                  CH.sub.3 H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  CH.sub.3 H        H       CH.sub.3                                                                               CH.sub.2 OH                                  NO.sub.2 H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  CH.sub.3 4-F      H       OCH.sub.3                                                                              CH.sub.2 OH                                  Cl       6-NO.sub.2                                                                              H       OCH.sub.3                                                                              CH.sub.2 OH                                  NO.sub.2 H        H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       6-F      H       CH.sub.3                                                                               CH.sub.2 OH                                  NO.sub.2 4-Cl     H       CH.sub.3                                                                               CH.sub.2 OH                                  Cl       5-OCH.sub.3                                                                             H       OCH.sub.3                                                                              CH.sub.2 OH                                  F        H        H       CH.sub.3                                                                               CH.sub.2 OH                                  H        H        H       CH.sub.3                                                                               CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                              H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                               OCH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3                                                                               H        H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                  OSO.sub.2 CH.sub.3                                                                      H        H       CH.sub.3                                                                               CH.sub.2 OH                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                             H        H       OCH.sub.3                                                                              CH.sub.2 OH                                  ______________________________________                                    

                                      TABLE 3h                                     __________________________________________________________________________      ##STR68##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X     Y           m.p. (°C.)                             __________________________________________________________________________     Cl     H    CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                  Br     H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      F      H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SC.sub.2 H.sub.5                                 H      H    H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               Cl     3-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                         CH.sub.3                                                                              H    H  OCH.sub.3                                                                            CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                      CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                        NO.sub.2                                                                              H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                CH.sub.3                                                                              4-F  H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      NO.sub.2                                                                              H    H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOC.sub.2 H.sub.5                               Cl     6-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7                     NO.sub.2                                                                              4-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 F      H    H  CH.sub.3                                                                             CH(SCH(CH.sub.3)CH.sub.2 S)                               H      H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                                SO.sub.2 N(CH.sub.3).sub.2                                                            H    CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                    OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7                         OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      SO.sub.2 -n-C.sub.3 H.sub. 7                                                          H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                NO.sub.2                                                                              H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                         Cl     H    H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.2 CH.sub.2 S)                         OSO.sub.2 CH.sub.3                                                                    H    H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                SO.sub.2 -n-C.sub.3 H.sub.7                                                           H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                                CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                                Br     H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                                Br     H    H  CH.sub.3                                                                             CH(CH.sub.3)(S(O)CH.sub.3)                                __________________________________________________________________________

                                      TABLE 4a                                     __________________________________________________________________________      ##STR69##                                                                     R.sub.16 R.sub.17                                                                            R.sub.21                                                                          X     Y        m.p. (°C.)                              __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Cl       H    H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                       H    H  Cl    CH(OCH.sub.3).sub.2                                     Cl       H    CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     H        H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2 H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2 6-Br H  CH.sub.3                                                                             CH(OCH.sub.3 ).sub.2                                    Cl       4-Cl H  Cl    CH(OCH.sub.3).sub.2                                     CF.sub.3 H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl       6-CH.sub.3                                                                          CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                      H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       4-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       6-F  H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 .sub.-n-C.sub.4 H.sub.9                                                        H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                        H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SCH.sub.3                                                                               H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     S(O).sub.2 CH.sub.3                                                                     H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SCH.sub.2 CH.sub.3                                                                      H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                    H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl       H    H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                            NO.sub.2 H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 C.sub.2 H.sub.5                                                                H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            __________________________________________________________________________

                                      TABLE 4b                                     __________________________________________________________________________      ##STR70##                                                                     R.sub.16  R.sub.17                                                                            R.sub.21                                                                           X     Y     m.p. (°C.)                               __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         Cl        H    H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                         Cl        H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         H         H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F  H   CH.sub.3                                                                             CH.sub.2 OTHP                                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         NO.sub.2  H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         NO.sub.2  6-Br H   CH.sub.3                                                                             CH.sub.2 OTHP                                         Cl        4-Cl H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         CF.sub.3  H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         Cl        6-CH.sub.3                                                                          H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         C.sub.2 H.sub.5                                                                          H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         CH(CH.sub.3).sub.2                                                                       H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 CH.sub.3                                                                        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                         H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         SO.sub.2 CH.sub.3                                                                        6-F  H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         SO.sub.2 -n-C.sub.4 H.sub.9                                                              H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 N(CH.sub.3).sub.2                                                               H    CH.sub.3                                                                           OCH.sub.3                                                                            CH.sub.2 OTHP                                         SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 -n-C.sub.3 H.sub.7                                                              H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H    H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OTHP                                         SCH.sub.3 H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         S(O).sub.2 CH.sub.3                                                                      H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SCH.sub.2 CH.sub.3                                                                       H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         __________________________________________________________________________

                  TABLE 4c                                                         ______________________________________                                          ##STR71##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 4d                                     __________________________________________________________________________      ##STR72##                                                                     R.sub.16 R.sub.17                                                                            R.sub.21                                                                          X     Y            m.p. (°C.)                          __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H    CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                    Cl       H    H  CH.sub.2 CH.sub.3                                                                    CH(OC.sub.2 H.sub.5).sub.2                              Cl       H    H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      H        H    H  OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                  CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                             CO.sub.2 CH(CH.sub.3).sub.2                                                             H    H  CH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                               NO.sub.2 H    H  CH.sub.3                                                                             CH(SCH.sub.2 CH.sub.2 S)                                NO.sub.2 6-Br H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub. 5                            Cl       4-Cl H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       CF.sub.3 H    CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2)                               Cl       6-CH.sub.3                                                                          H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      C.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                    CH(CH.sub.3).sub.2                                                                      H    H  CH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3).sub.2                           SO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                       4-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                    SO.sub.2 CH.sub.3                                                                       6-F  H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                               SO.sub.2 -n-C.sub.4 H.sub.9                                                             H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7                   SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H    H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    H  CH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)            SO.sub.2 -n-C.sub.3 H.sub.7                                                             H    H  CH.sub.3                                                                             CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                    SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                        H    H  OCH.sub.3                                                                            CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                     SCH.sub.3                                                                               H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              S(O).sub.2 CH.sub.3                                                                     H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              SCH.sub.2 CH.sub.3                                                                      H    H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7              S(O).sub.2 -n-C.sub.4 H.sub.9                                                           H    CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      Cl       H    H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.3).sub.2                            CH.sub.3 H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                       SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                              SCH.sub.3                                                                               H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                     SCH.sub.3                                                                               H    H  OCH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                   __________________________________________________________________________

                                      TABLE 4e                                     __________________________________________________________________________      ##STR73##                                                                     R.sub.16 R.sub.17                                                                            R.sub.21                                                                          X     Y        m.p. (°C.)                              __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Cl       H    H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                     Cl       H    CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     H        H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2 H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2 6-Br H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CF.sub.3 H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl       6-CH.sub.3                                                                          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                      H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       4-OCH.sub.3                                                                         H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       6-F  H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.4 H.sub.9                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                        H    H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SCH.sub.3                                                                               H    CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     S(O).sub.2 CH.sub.3                                                                     H    H  CH.sub. 3                                                                            CH(OCH.sub.3).sub.2                                     SCH.sub.2 CH.sub.3                                                                      H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                    H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CF.sub.3 H    H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                            Cl       H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            NO.sub.2 H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.2 CH.sub.3                                                              H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            __________________________________________________________________________

                                      TABLE 4f                                     __________________________________________________________________________      ##STR74##                                                                     R.sub.16  R.sub.17                                                                            R.sub.21                                                                           X     Y     m.p. (°C.)                               __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         Cl        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         Cl        H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         H         H    H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OTHP                                         CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F  H   CH.sub.3                                                                             CH.sub.2 OTHP                                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         NO.sub.2  H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         NO.sub.2  6-Br H   CH.sub.3                                                                             CH.sub.2 OTHP                                         Cl        4-Cl H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         CF.sub.3  H    CH.sub.3                                                                           OCH.sub.3                                                                            CH.sub.2 OTHP                                         Cl        6-CH.sub.3                                                                          H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OTHP                                         C.sub.2 H.sub.5                                                                          H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         CH(CH.sub.3).sub.2                                                                       H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 CH.sub.3                                                                        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                         H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         SO.sub.2 CH.sub.3                                                                        6-F  H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         SO.sub.2 -n-C.sub.4 H.sub.9                                                              H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 N(CH.sub.3).sub.2                                                               H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 -n-C.sub.3 H.sub.7                                                              H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         SCH.sub.3 H    H   CH.sub.3                                                                             CH.sub.2 OTHP                                         S(O).sub.2 CH.sub.3                                                                      H    H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                         SCH.sub.2 CH.sub.3                                                                       H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H    H   OCH.sub.3                                                                            CH.sub.2 OTHP                                         __________________________________________________________________________

                  TABLE 4g                                                         ______________________________________                                          ##STR75##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub. 2 OH                                CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2  -n-C.sub.4 H.sub.9                                                              H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.2 CH.sub. 3                                                                    CH.sub.2 OH                                 S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 4h                                     __________________________________________________________________________      ##STR76##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y             m.p. (°C.)                     __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        4-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.2 CH.sub.3                                                                    CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub. 3 H.sub.7                                                             H     H   CH.sub.3                                                                              CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7          S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  NO.sub.2  H     H   CH.sub.3                                                                              CH(CH.sub.3)(SCH.sub.3).sub.2                       Cl        H     H   CH.sub.3                                                                              CH(CH.sub.3)(SO.sub.2 CH.sub.3)                     CF.sub.3  H     H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                          CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   CH.sub.3                                                                              CH(SCH.sub.3).sub.2                                 CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   OCH.sub.3                                                                             CH.sub.2 S(O)CH.sub.2 CH.sub.3                      CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   CH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                               __________________________________________________________________________

                                      TABLE 5a                                     __________________________________________________________________________      ##STR77##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y           m.p. (°C.)                       __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 Cl        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CO.sub.2 CH.sub.3                                                                        H     CH.sub.3                                                                           Cl     CH(OCH.sub.3).sub.2                                 Cl        H     H   OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                 H         H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 NO.sub.2  H     H   CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                                 NO.sub.2  6-Br  H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 Cl        4-Cl  H   Cl     CH(OCH.sub.3).sub.2                                 CF.sub.3  H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO -n-C.sub.4 H.sub.9                                                                    H     CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CH.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2               SCH.sub.3 H     H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        NO.sub.2  H     H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        CO.sub.2 CH.sub.3                                                                        H     H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                        SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                     H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 __________________________________________________________________________

                  TABLE 5b                                                         ______________________________________                                          ##STR78##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub. 2 OTHP                              Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                               C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               CH(CH.sub.3).sub.2                                                                        H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               S(O).sub.2 - n-C.sub.4 H.sub.9                                                            H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 5c                                                         ______________________________________                                          ##STR79##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub. 2 OH                                Cl         6-CH.sub.3                                                                              H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 5d                                     __________________________________________________________________________      ##STR80##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y             m.p. (°C.)                     __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                Cl        H     CH.sub.3                                                                           CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  H   CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        4-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH.sub. 2 OCO .sub.-i-C.sub.3 H.sub.7               SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     CH.sub.3                                                                           CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7          S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   CH.sub.3                                                                              C(CH.sub.3)(OC.sub.2 H.sub.5).sub.2                 CF.sub.3  H     H   CH.sub.3                                                                              CH(CH.sub.3)SC.sub.2 H.sub.5                        SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                          SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                               SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(CH.sub.3)(S(O)CH.sub.3)                          __________________________________________________________________________

                  TABLE 5e                                                         ______________________________________                                          ##STR81##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21 X  Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            Cl         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            Cl         H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            H          H        CH.sub.3 OCH.sub.3                                                                         CH(OCH.sub.3).sub.2                            CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      HCH.sub.3   CH(OCH.sub.3).sub.2                            CO.sub.2 CH(CH.sub.3).sub.2                                                               H        HCH.sub.3   CH(OCH.sub.3).sub.2                            NO.sub.2   H        HCH.sub.3   CH(OCH.sub.3).sub.2                            NO.sub.2   6-Br     HCH.sub.3   CH(OCH.sub.3).sub.2                            CF.sub. 3  H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            Cl         6-CH.sub.3                                                                              HOCH.sub.3  CH(OCH.sub.3).sub.2                            C.sub.2 H.sub.5                                                                           H        HCH.sub.3   CH(OCH.sub.3).sub.2                            CH(CH.sub.3).sub.2                                                                        H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                         6-F      HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3).sub.2                                                                H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        HCH.sub.2 CH.sub.3                                                                         CH(OCH.sub.3).sub.2                            SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            SCH.sub.3  H        HCH.sub.3   CH(OCH.sub.3).sub.2                            S(O).sub.2 CH.sub.3                                                                       H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SCH.sub.2 CH.sub.3                                                                        H        HOCH.sub.2 CH.sub.3                                                                        CH(OCH.sub.3).sub.2                            S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                      H        CH.sub.3 OCH.sub.3                                                                         CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.2 CH.sub.3                                                                H        HOCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                   CH.sub.3   H        HOCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                   CO.sub.2 CH.sub.3                                                                         H        HOCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                   ______________________________________                                    

                  TABLE 5f                                                         ______________________________________                                          ##STR82##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTP                                H          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CF.sub.3   H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                               Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                               C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 5g                                                         ______________________________________                                          ##STR83##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub. 3  H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 H-n-C.sub.4 H.sub.9                                                                     H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 5h                                     __________________________________________________________________________      ##STR84##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y             m.p. (°C.)                     __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  H   CH.sub.3                                                                              CH.sub.2 OCOC.sub. 2 H.sub.5                        Cl        4-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub.3 H.sub. 7                                                             H     H   CH.sub.3                                                                              CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7          S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  SO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   OCH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                 Cl        H     H   OCH.sub.3                                                                             C(C.sub.2 H.sub.5)(OCH.sub.2 CH.sub.2 O)            NO.sub.2  H     H   OCH.sub.3                                                                             C(CH.sub.3)(SCH.sub.3).sub.2                        NO.sub.2  H     H   OCH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                               __________________________________________________________________________

                  TABLE 6a                                                         ______________________________________                                          ##STR85##                                                                                                               m.p.                                 R.sub.16   R.sub.17                                                                               R.sub.21                                                                              X       Y       (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          Cl         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.3                                                                         H       H      Cl      CH(OCH.sub.3).sub.2                          Cl         H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          H          H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          NO.sub.2   H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          NO.sub.2   6-Br    H      CH.sub.3                                                                               CH(OCH.sub. 3).sub.2                         CF.sub.3   H       H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                          Cl         6-CH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          C.sub.2 H.sub.5                                                                           H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CH(CH.sub.3).sub.2                                                                        H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                         6-F     H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.4 H.sub.9                                                               H       CH.sub.3                                                                              CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                                H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.3 H.sub.7                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SCH.sub.3  H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          S(O).sub.2 CH.sub.3                                                                       H       H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                          SCH.sub.2 CH.sub. 3                                                                       H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                      H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CH.sub.3   H       H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                 CO.sub.2 CH.sub.2 CH.sub.3                                                                H       H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                 SCH.sub.3  H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 Cl         H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 ______________________________________                                    

                  TABLE 6b                                                         ______________________________________                                          ##STR86##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H          H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         2-Cl     H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CF.sub.3   H        H      OCH.sub. 3                                                                             CH.sub.2 OTHP                               Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                               C.sub.2 H.sub.5                                                                           H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               S(O).sub.2 H-n-C.sub.4 H.sub.9                                                                     H      OCH.sub.3                                                                              CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 6c                                                         ______________________________________                                          ##STR87##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         2-Cl     H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 H-n-C.sub.4 H.sub.9                                                                     H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 6d                                     __________________________________________________________________________      ##STR88##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y             m.p. (°C.)                     __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  H   CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        2-Cl  H   OCH.sub. 3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        5-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7          S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 SCH.sub.3                                  CH.sub.3  H     H   OCH.sub.3                                                                             CH(SCH.sub.2 CH.sub.3).sub.2                        NO.sub.2  H     H   OCH.sub.3                                                                             CH(SCH.sub.3).sub.2                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   C.sub.2 H.sub.5                                                                       CH.sub.2 SO.sub.2 CH.sub.3                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                               SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   CH.sub.3                                                                              CH.sub.2 S(O)CH.sub.2 CH.sub.3                      __________________________________________________________________________

                                      TABLE 6e                                     __________________________________________________________________________      ##STR89##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y           m.p. (°C.)                       __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 Cl        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 Cl        H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 H         H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 NO.sub.2  6-Br  H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CF.sub.3  H     H   OCH.sub. 3                                                                            CH(OCH.sub.3).sub.2                                 Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                        5-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     CH.sub.3                                                                           CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                 S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OCH.sub.3 ).sub.2                                SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                     H     H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                 CH(CH.sub.3).sub.2                                                                       H     H   OCH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2               CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   OCH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2               CF.sub.3  H     H   OCH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2               __________________________________________________________________________

                  TABLE 6f                                                         ______________________________________                                          ##STR90##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               CO.sub.2 CH(CH.sub.3).sub.2                                                               H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         2-Cl     H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                               C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 6g                                                         ______________________________________                                          ##STR91##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         2-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub. 2 OH                                S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 6h                                     __________________________________________________________________________      ##STR92##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y             m.p. (°C.)                     __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  H   CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        2-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        5-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH.sub. 2 OCO .sub.-i-C.sub.3 H.sub.7               SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7          S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  SCH.sub.2 CH.sub.3                                                                       H     H   OC.sub.2 H.sub.5                                                                      C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)          Cl        H     H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                          CH.sub.3  H     H   OCH.sub.3                                                                             CH(SCH.sub.2 CH.sub.3).sub.2                        __________________________________________________________________________

                                      TABLE 7a                                     __________________________________________________________________________      ##STR93##                                                                     R.sub.17                                                                             R.sub.18    R.sub.21                                                                           X      Y           m.p. (°C.)                     __________________________________________________________________________     H     CO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               4-CH.sub.3                                                                           CO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     CO.sub.2 CH.sub.3                                                                          H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     H           H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     SCH.sub.2 CH.sub.2 CH.sub.3                                                                H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SCH.sub.3   H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     CH(CH.sub.3).sub.2                                                                         H   OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                               H     CH.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     F           H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     Cl          H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               5-Cl  Cl          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     Br          CH.sub.3                                                                           OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     NO.sub.2    H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     SO.sub.2 N(CH.sub.3).sub.2                                                                 H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     OCH.sub.3   CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               5-OCH.sub.3                                                                          OCH.sub.3   H   CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                               5-F   O(CH.sub.2).sub.3 CH.sub.3                                                                 H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               4-Br  SO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     CO.sub.2 CH.sub.3                                                                          H   Cl     CH(OCH.sub.3).sub.2                               H     NO.sub.2    H   Cl     CH(OCH.sub.3).sub.2                               H     Cl          H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                      H     CO.sub.2 CH.sub.3                                                                          H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                      H     CO.sub.2 CH.sub.3                                                                          H   OCH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2             H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H   Cl     CH(OCH.sub.3).sub.2                               H     SO.sub.2 CH.sub.3                                                                          H   Cl     CH(OCH.sub.3).sub.2                               H     SCH.sub.3   H   Cl     CH(OCH.sub.3).sub.2                               __________________________________________________________________________

                  TABLE 7b                                                         ______________________________________                                          ##STR94##                                                                                                          m.p.                                      R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y (°C.)                            ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      H              H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CH.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      F              H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      Cl             H      OCH.sub.3                                                                              CH.sub.2 OTHP                             5-Cl   Cl             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      Br             CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                             H      NO.sub.2       CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                             H      OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-Br   SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             ______________________________________                                    

                  TABLE 7c                                                         ______________________________________                                          ##STR95##                                                                                                         m.p.                                       R.sub.17                                                                              R.sub.18      R.sub.21                                                                              X       Y(°C.)                              ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OH 143-                                                               147°                                4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OH                                H      CO.sub.2 CH.sub.2 CH                                                                         H      OCH.sub.3                                                                              CH.sub.2 OH                                H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                 H      CH.sub.3                                                                               CH.sub.2 OH                                H      H             H      CH.sub.3                                                                               CH.sub.2 OH                                H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                  H      OCH.sub.3                                                                              CH.sub.2 OH                                H      SCH.sub.3     H      CH.sub.3                                                                               CH.sub.2 OH                                H      CH(CH.sub.3).sub.2                                                                           H      OCH.sub.3                                                                              CH.sub.2 OH                                H      CH.sub.2 CH.sub.3                                                                            CH.sub.3                                                                              CH.sub.3                                                                               CH.sub. 2 OH                               H      F             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                H      Cl            CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                5-Cl   Cl            H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                H      Br            H      OCH.sub.3                                                                              CH.sub.2 OH                                H      NO.sub.2      H      CH.sub.3                                                                               CH.sub.2 OH                                H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H     CH.sub.3                                                                               CH.sub.2 OH                                H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H     OCH.sub.3                                                                              CH.sub.2 OH                                H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H     OCH.sub.3                                                                              CH.sub.2 OH                                H      OCH.sub.3      H     CH.sub.3                                                                               CH.sub.2 OH                                5-OCH.sub.3                                                                           OCH.sub.3      H     CH.sub.3                                                                               CH.sub.2 OH                                5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H     OCH.sub.3                                                                              CH.sub.2 OH                                H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H     OCH.sub.3                                                                              CH.sub.2 OH                                H      SO.sub.2 CH.sub.3                                                                             H     CH.sub.3                                                                               CH.sub.2 OH                                4-Br   SO.sub.2 CH.sub.3                                                                             H     CH.sub.3                                                                               CH.sub.2 OH                                ______________________________________                                    

                                      TABLE 7d                                     __________________________________________________________________________      ##STR96##                                                                     R.sub.17                                                                             R.sub.18   R.sub.21                                                                           X      Y            m.p. (°C.)                     __________________________________________________________________________     H     CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                         4-CH.sub.3                                                                           CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     CO.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                 H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H   CH.sub.3                                                                              CH.sub.2 OCONHCH.sub.3                             H     H          H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                        H     SCH.sub.2 CH.sub.2 CH.sub.3                                                               H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                          H     SCH.sub.3  H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                           H     CH(CH.sub.3).sub.2                                                                        H   OCH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                        H     CH.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH(OCH(CH.sub.3)CH.sub.2 O)                        H     F          H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                  H     Cl         H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                 5-Cl  Cl         H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     Br         CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3).sub.2                      H     NO.sub.2   CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                           H     SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                       H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 SCH.sub.2 CH.sub.3                        H     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                         H     OCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                 5-OCH.sub.3                                                                          OCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2               5-F   O(CH.sub.2).sub.3 CH.sub.3                                                                H   OCH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2               H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H   CH.sub.3                                                                              CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)             H     SO.sub.2 CH.sub.3                                                                         H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                H     SCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                         H     CH.sub.3   H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                H     CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                         __________________________________________________________________________

                  TABLE 7e                                                         ______________________________________                                          ##STR97##                                                                                                         m.p.                                       R.sub.17                                                                              R.sub.18      R.sub.21                                                                              X       Y (°C.)                             ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      CO.sub.2 CH.sub.3                                                                            H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                        H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                 H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      H             CH.sub.3                                                                              CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                  H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      SCH.sub.3     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      CH(CH.sub.3).sub.2                                                                           H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      CH.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      F             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      Cl            H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        5-Cl   Cl            H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      Br            H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      NO.sub.2      H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H     CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      SO.sub.2 N(CH.sub.3).sub.2                                                                   CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      OCH.sub.3     H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                        5-OCH.sub.3                                                                           OCH.sub.3     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                          H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                        H      SO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        4-Br   SO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                        H      Cl            H      CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                 H      Br            H      OCH.sub.3                                                                            C(CH.sub.3 )(OCH.sub.3).sub.2                H      SO.sub.2 CH.sub.3                                                                            H      OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                 H      CO.sub.2 CH.sub.3                                                                            H      OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                 ______________________________________                                    

                  TABLE 7f                                                         ______________________________________                                          ##STR98##                                                                                                          m.p.                                      R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y (°C.)                            ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                             H      H              H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CH.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      F              H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                             H      Cl             H      OCH.sub.3                                                                              CH.sub.2 OTHP                             5-Cl   Cl             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      Br             CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                             H      NO.sub.2       H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-Br   SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             ______________________________________                                    

                  TABLE 7g                                                         ______________________________________                                          ##STR99##                                                                                                          m.p.                                      R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y (°C.)                            ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OH                               4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OH                               H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                               H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.3                                                                               CH.sub.2 OH                               H      H              H      CH.sub.3                                                                               CH.sub.2 OH                               H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OH                               H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OH                               H      CH.sub.2 CH.sub.3                                                                             H      CH.sub. 3                                                                              CH.sub.2 OH                               H      F              H      OCH.sub.3                                                                              CH.sub.2 OH                               H      Cl             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                               5-Cl   Cl             H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                               H      Br             H      OCH.sub.3                                                                              CH.sub.2 OH                               H      NO.sub.2       H      CH.sub.3                                                                               CH.sub.2 OH                               H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H      CH.sub.3                                                                               CH.sub.2 OH                               H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.3                                                                              CH.sub.2 OH                               H      OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OH                               5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OH                               5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OH                               4-Br   SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OH                               ______________________________________                                    

                                      TABLE 7h                                     __________________________________________________________________________      ##STR100##                                                                    R.sub.17                                                                             R.sub.18   R.sub.21                                                                           X      Y             m.p. (°C.)                    __________________________________________________________________________     H     CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                         4-CH.sub.3                                                                           CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     CO.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                 H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H   CH.sub.3                                                                              CH.sub.2 OCONHCH.sub.3                             H     H          H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                        H     SCH.sub.2 CH.sub.2 CH.sub.3                                                               H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                          H     SCH.sub.3  H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                           H     CH(CH.sub.3).sub.2                                                                        H   OCH.sub.3                                                                             CH.sub. 2 OCOC.sub.2 H.sub.5                       H     CH.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH(CH.sub.3)CH.sub.2 O)                        H     F          H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                  H     Cl         H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                 5-Cl  Cl         H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCOCH.sub.3                               H     Br         H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCON(CH.sub.3).sub.2                      H     NO.sub.2   H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                           H     SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                       H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.2 CH.sub.3                        H     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                         H     OCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                 5-OCH.sub.3                                                                          OCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2               5-F   O(CH.sub.2).sub.3 CH.sub.3                                                                H   OCH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2               H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H   CH.sub.3                                                                              CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)             H     SO.sub.2 CH.sub. 3                                                                        H   CH.sub.3                                                                              CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                H     CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)         H     CO.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                             C(CH.sub.3)(SCH.sub.3).sub.2                       H     CO.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                             CH(SCH.sub.3).sub.2                                H     Cl         H   OCH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                __________________________________________________________________________

                                      TABLE 8a                                     __________________________________________________________________________      ##STR101##                                                                    R.sub.17                                                                              R.sub.18     R.sub.21                                                                            X       Y         m.p. (°C.)                   __________________________________________________________________________     H      CO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.3                                                                           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.2CH.sub.2                                                                   H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      H            H    CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                 H    OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           H      SCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CH(CH.sub.3).sub.2                                                                          H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      CH.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      F            H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      Cl           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           5-Cl   Cl           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      Br           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      NO.sub.2     H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                       H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(CH.sub.3).sub.2                                                                  H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                               H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      OCH.sub.3    CH.sub.3                                                                            CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           5-OCH.sub.3                                                                           OCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                  H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                         H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           4-Br   SO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.3                                                                           H    Cl      CH(OCH.sub.3).sub.2                           H      NO.sub.2     H    Cl      CH(OCH.sub.3).sub.2                           H      CH.sub.3     H    CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  H      CH.sub.3     H    OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  H      SCH.sub.3    H    CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  H      Br           H    OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                         H    Cl      CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.3                                                                           H    Cl      CH(OCH.sub.3).sub.2                           H      SCH.sub.3    H    Cl      CH(OCH.sub.3).sub.2                           H      SO.sub.2 -n-C.sub.3 H.sub.7                                                                 H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                                                                      121-124° d                   __________________________________________________________________________

                  TABLE 8b                                                         ______________________________________                                          ##STR102##                                                                                                              m.p.                                 R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y    (°C.)                         ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      H              H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CH.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      F              H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      Cl             H      OCH.sub.3                                                                              CH.sub.2 OTHP                             5-Cl   Cl             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      Br             H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      NO.sub.2       CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.3                                                                             H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                             4-Br   SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             ______________________________________                                    

                  TABLE 8c                                                         ______________________________________                                          ##STR103##                                                                                                              m.p.                                 R.sub.17                                                                              R.sub.18       R.sub.21                                                                               X       Y   (°C.)                         ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H       CH.sub.3                                                                               CH.sub.2 OH                              4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                              H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H       OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                              H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H       CH.sub.3                                                                               CH.sub.2 OH                              H      H              H       CH.sub.3                                                                               CH.sub.2 OH                              H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H       OCH.sub.3                                                                              CH.sub.2 OH                              H      SCH.sub.3      CH.sub.3                                                                               CH.sub.3                                                                               CH.sub.2 OH                              H      CH(CH.sub.3).sub.2                                                                            H       OCH.sub.3                                                                              CH.sub.2 OH                              H      CH.sub.2 CH.sub.3                                                                             H       CH.sub. 3                                                                              CH.sub.2 OH                              H      F              H       OCH.sub.3                                                                              CH.sub.2 OH                              H      Cl             H       OCH.sub.3                                                                              CH.sub.2 OH                              5-Cl   Cl             H       CH.sub.3                                                                               CH.sub.2 OH                              H      Br             H       OCH.sub.3                                                                              CH.sub.2 OH                              H      NO.sub.2       H       CH.sub.3                                                                               CH.sub.2 OH                              H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H       CH.sub.3                                                                               CH.sub.2 OH                              H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H       OCH.sub.3                                                                              CH.sub.2 OH                              H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H       OCH.sub.3                                                                              CH.sub.2 OH                              H      OCH.sub.3      H       CH.sub.3                                                                               CH.sub.2 OH                              5-OCH.sub.3                                                                           OCH.sub.3      H       CH.sub.3                                                                               CH.sub.2 OH                              5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H       OCH.sub.3                                                                              CH.sub.2 OH                              H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H       OCH.sub.3                                                                              CH.sub.2 OH                              H      SO.sub.2 CH.sub.3                                                                             H       CH.sub.3                                                                               CH.sub.2 OH                              4-Br   SO.sub.2 CH.sub.3                                                                             H       CH.sub.3                                                                               CH.sub.2 OH                              ______________________________________                                    

                                      TABLE 8d                                     __________________________________________________________________________      ##STR104##                                                                    R.sub.17                                                                              R.sub.18    R.sub.21                                                                            X       Y            m.p. (°C.)                 __________________________________________________________________________     H      CO.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                     4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH.sub.2 OCOCH.sub.3                           H      CO.sub.2 CH.sub.3                                                                          H    OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H    CH.sub.3                                                                               CH.sub.2 OCONHCH.sub.3                         H      H           H    CH.sub.3                                                                               CH.sub.2 OCO.sub.2 CH.sub.3                    H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                H    OCH.sub.2 CH.sub.3                                                                     CH.sub.2 SC.sub.2 H.sub.5                      H      SCH.sub.3   H    CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.2 CH.sub.2 O)                       H      CH(CH.sub.3).sub.2                                                                         H    OCH.sub. 3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                    H      CH.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH(OCH(CH.sub.3)CH.sub.2 O)                    H      F           H    OCH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)              H      Cl          H    OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                             5-Cl   Cl          H    CH.sub.3                                                                               CH.sub.2 OCOCH.sub.3                           H      Br          H    OCH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                  H      NO.sub.2    H    CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                       H      SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        H    CH.sub.3                                                                               CH.sub.2 OCOCH.sub.3                           H      SO.sub.2 N(CH.sub.3).sub.2                                                                 H    OCH.sub.3                                                                              CH.sub.2 SCH.sub.2 CH.sub.3                    H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H    CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                     H      OCH.sub.3   CH.sub.3                                                                            CH.sub.3                                                                               CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5             5-OCH.sub.3                                                                           OCH.sub.3   H    CH.sub.3                                                                               CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2           5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                 H    OCH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2           H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H    CH.sub.3                                                                               CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)         H      SO.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)            H      Cl          H    CH.sub.3                                                                               CH.sub.2 SO.sub.2 CH.sub.3                     H      Br          H    CH.sub.3                                                                               CH(SCH.sub.3).sub.2                            H      F           H    CH.sub.3                                                                               CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3            H      SO.sub.2 N(CH.sub.3).sub.2                                                                 H    OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.2 CH.sub.3).sub.2          __________________________________________________________________________

                                      TABLE 8e                                     __________________________________________________________________________      ##STR105##                                                                    R.sub.17                                                                              R.sub.18     R.sub.21                                                                            X       Y           m.p. (°C.)                 __________________________________________________________________________     H      CO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.3                                                                           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      H            H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                 H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CH(CH.sub.3).sub.2                                                                          H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      CH.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      F            H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      Cl           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           5-Cl   Cl           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      Br           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      NO.sub.2     H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                       H    CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(CH.sub.3).sub.2                                                                  H    OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                               CH.sub.3                                                                            OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      OCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           5-OCH.sub.3                                                                           OCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                  H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                         H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           4-Br   SO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      OCH.sub.3    H    CH.sub.2 CH.sub.3                                                                      C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2         H      SCH.sub.3    H    CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  H      CH.sub.2 CH.sub.3                                                                           H    OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  H      CH.sub.3     H    OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  __________________________________________________________________________

                  TABLE 8f                                                         ______________________________________                                          ##STR106##                                                                                                              m.p.                                 R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y    (°C.)                         ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      H              H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CH.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      F              H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      Cl             CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                             5-Cl   Cl             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      Br             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                             H      NO.sub.2       H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             4-Br   SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             ______________________________________                                    

                  TABLE 8g                                                         ______________________________________                                          ##STR107##                                                                                                              m.p.                                 R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y    (°C.)                         ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OH                               4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                               H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                               H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.3                                                                               CH.sub.2 OH                               H      H              H      CH.sub.3                                                                               CH.sub.2 OH                               H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OH                               H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OH                               H      CH.sub. 2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OH                               H      F              H      OCH.sub.3                                                                              CH.sub.2 OH                               H      Cl             H      OCH.sub.3                                                                              CH.sub.2 OH                               5-Cl   Cl             H      CH.sub.3                                                                               CH.sub.2 OH                               H      Br             H      OCH.sub.3                                                                              CH.sub.2 OH                               H      NO.sub.2       H      CH.sub.3                                                                               CH.sub.2 OH                               H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H      CH.sub.3                                                                               CH.sub.2 OH                               H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.3                                                                              CH.sub.2 OH                               H      OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OH                               5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OH                               5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OH                               H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                               H      SO.sub.2 CH.sub.3                                                                             CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                               4-Br   SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OH                               ______________________________________                                    

                                      TABLE 8h                                     __________________________________________________________________________      ##STR108##                                                                    R.sub.17                                                                              R.sub.18    R.sub.21                                                                            X       Y             m.p. (°C.)                __________________________________________________________________________     H      CO.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                     4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH.sub.2 OCOCH.sub.3                           H      CO.sub.2 CH.sub.3                                                                          CH.sub.3                                                                            OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                               CH.sub.3                                                                            CH.sub.3                                                                               CH.sub.2 OCONHCH.sub.3                         H      H           H    CH.sub.3                                                                               CH.sub.2 OCO.sub.2 CH.sub.3                    H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                H    OCH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                      H      SCH.sub.3   H    CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                       H      CH(CH.sub.3).sub. 2                                                                        H    OCH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                    H      CH.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               CH(OCH(CH.sub.3)CH.sub.2 O)                    H      F           H    OCH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)              H      Cl          H    OCH.sub.2 CH.sub.3                                                                     CH.sub.2 SCH.sub.3                             5-Cl   Cl          H    CH.sub.2 CH.sub.3                                                                      CH.sub.2 OCOCH.sub.3                           H      Br          H    OCH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                  H      NO.sub.2    H    CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                       H      SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        H    CH.sub.3                                                                               CH.sub.2 OCOCH.sub.3                           H      SO.sub.2 N(CH.sub.3).sub.2                                                                 H    OCH.sub.3                                                                              CH.sub.2 SCH.sub.2 CH.sub.3                    H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H    CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                     H      OCH.sub.3   H    CH.sub.3                                                                               CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5             5-OCH.sub.3                                                                           OCH.sub.3   H    CH.sub.3                                                                               CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2           5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                 H    OCH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2           H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H    CH.sub.3                                                                               CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)         H      SO.sub. 2 CH.sub.3                                                                         H    CH.sub.3                                                                               CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)            H      Br          H    OCH.sub.3                                                                              C(CH.sub.3)(SCH.sub.3).sub.2                   H      NO.sub.2    H    OCH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                     H      SO.sub.2 CH.sub.2 CH.sub.3                                                                 H    OCH.sub.3                                                                              CH(CH.sub.3)SCH.sub.3                          H      CO.sub.2 CH.sub.3                                                                          H    CH.sub.3                                                                               C(CH.sub.2 CH.sub.3)(OCH.sub.2 CH.sub.2        __________________________________________________________________________                                     O)                                        

                                      TABLE 9a                                     __________________________________________________________________________      ##STR109##                                                                    R.sub.17                                                                              R.sub.18     R.sub.21                                                                            X       Y         m.p. (°C.)                   __________________________________________________________________________     H      CO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.3                                                                           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      H            H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                 H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CH(CH.sub.3).sub.2                                                                          H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      CH.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      F            CH.sub.3                                                                            OCH.sub.3                                                                              CH(OCH.sub.3 ).sub.2                          H      Cl           H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           5-Cl   Cl           CH.sub.3                                                                            CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      Br           H    OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           H      NO.sub.2     H    CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                       H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(CH.sub.3).sub.2                                                                  H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                               H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      OCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           5-OCH.sub.3                                                                           OCH.sub.3    H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                  H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                         H    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.3                                                                           H    CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.3                                                                           H    Cl      CH(OCH.sub.3).sub.2                           H      NO.sub.2     H    Cl      CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                         H    Cl      CH(OCH.sub.3).sub.2                           H      SO.sub.2 CH.sub.3                                                                           H    Cl      CH(OCH.sub.3).sub.2                           H      SCH.sub.3    H    Cl      CH(OCH.sub.3).sub.2                           H      CO.sub.2 CH.sub.3                                                                           H    OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  H      SO.sub.2 CH.sub.3                                                                           H    OC.sub.2 H.sub.5                                                                       C(CH.sub.3)(OCH.sub.3).sub.2                  H      Br           H    CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  H      F            CH.sub.3                                                                            OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                  __________________________________________________________________________

                  TABLE 9b                                                         ______________________________________                                          ##STR110##                                                                                                              m.p.                                 R.sub.17                                                                              R.sub.18       R.sub.21                                                                              X       Y    (°C.)                         ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      H              H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      CH(CH.sub.3).sub.2                                                                            H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      CH.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      F              H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      Cl             H      OCH.sub. 2 CH.sub.3                                                                    CH.sub.2 OTHP                             5-Cl   Cl             H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                             H      Br             H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      NO.sub.2       H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         H      CH.sub.3                                                                               CH.sub.2 OTHP                             H      SO.sub.2 N(CH.sub.3).sub.2                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      OCH.sub.3      CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                             5-OCH.sub.3                                                                           OCH.sub.3      H      CH.sub.3                                                                               CH.sub.2 OTHP                             5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           H      OCH.sub.3                                                                              CH.sub.2 OTHP                             H      SO.sub.2 CH.sub.3                                                                             H      CH.sub.3                                                                               CH.sub.2 OTHP                             ______________________________________                                    

                                      TABLE 9c                                     __________________________________________________________________________      ##STR111##                                                                    R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X     Y     m.p. (°C.)                              __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OH                                          H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                             CH.sub.2 OH                                          H    H           H  CH.sub.3                                                                             CH.sub.2 OH                                          H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SCH.sub.3   CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OH                                          H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OH                                          H    F           H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    Cl          H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OH                                          5-Cl Cl          H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                          H    Br          H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    NO.sub.2    H  CH.sub.3                                                                             CH.sub.2 OH                                          H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OH                                          H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    OCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OH                                          5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OH                                          5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OH                                          __________________________________________________________________________

                                      TABLE 9d                                     __________________________________________________________________________      ##STR112##                                                                    R.sub.17                                                                            R.sub.18  R.sub.21                                                                          X     Y            m.p. (°C.)                         __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    CO.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H  CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                 H    H         H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H    SCH.sub.2 CH.sub.2 CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                              H    SCH.sub.3 H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    CH(CH.sub.3).sub.2                                                                       H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                            H    CH.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OCH(CH.sub.3 )CH.sub.2 O)                           H    F         H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      H    Cl        H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SCH.sub.3                                     5-Cl Cl        H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOCH.sub.3                                   H    Br        CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                          H    NO.sub.2  H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                            H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                     5-OCH.sub.3                                                                         OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                               H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)                 H    SO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                    H    Cl        CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             H    CH.sub.3  H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             H    Br        H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             H    SCH.sub.3 H  OCH.sub.3                                                                            C(CH.sub.3)(OEt).sub.2                                 H    CO.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2                               O)                                                     __________________________________________________________________________

                                      TABLE 9e                                     __________________________________________________________________________      ##STR113##                                                                    R.sub.17                                                                            R.sub.18   R.sub.21                                                                          X     Y        m.p. (°C.)                            __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    H          H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SCH.sub.2 CH.sub.2 CH.sub.3                                                               CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CH(CH.sub.3).sub.2                                                                        H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                   H    CH.sub.2 CH.sub.3                                                                         H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub. 3).sub.2                                  H    F          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    Cl         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   5-Cl Cl         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Br         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                     H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-OCH.sub.3                                                                         OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.3                                                                H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          H    NO.sub.2   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3 ).sub.2                         H    SCH.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    Br         CH.sub.3                                                                          CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          __________________________________________________________________________

                                      TABLE 9f                                     __________________________________________________________________________      ##STR114##                                                                    R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X     Y     m.p. (°C.)                              __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OTHP                                        H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                             CH.sub.2 OTHP                                        H    H           H  CH.sub.3                                                                             CH.sub.2 OTHP                                        H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OTHP                                        H    SCH.sub.3   H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                        H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OTHP                                        H    F           H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    Cl          H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        5-Cl Cl          H  CH.sub.3                                                                             CH.sub.2 OTHP                                        H    Br          H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    NO.sub.2    CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OTHP                                        H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OTHP                                        H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    OCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OTHP                                        5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OTHP                                        5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                            CH.sub.2 OTHP                                        H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OTHP                                        __________________________________________________________________________

                                      TABLE 9g                                     __________________________________________________________________________      ##STR115##                                                                    R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X     Y     m.p. (°C.)                              __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OH                                          H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                             CH.sub.2 OH                                          H    H           H  CH.sub.3                                                                             CH.sub.2 OH                                          H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OH                                          H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OH                                          H    F           H  OCH.sub.3                                                                            CH.sub. 2 OH                                         H    Cl          H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OH                                          5-Cl Cl          H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                          H    Br          H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    NO.sub.2    H  CH.sub.3                                                                             CH.sub.2 OH                                          H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OH                                          H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    OCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OH                                          5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                             CH.sub.2 OH                                          5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                            CH.sub.2 OH                                          H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                             CH.sub.2 OH                                          __________________________________________________________________________

                                      TABLE 9h                                     __________________________________________________________________________      ##STR116##                                                                    R.sub.17                                                                            R.sub.18  R.sub.21                                                                          X     Y           m.p. (°C.)                          __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    CO.sub.2 CH.sub.3                                                                        CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H  CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                 H    H         H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H    SCH.sub.2 CH.sub.2 CH.sub.3                                                              H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SC.sub.2 H.sub.5                              H    SCH.sub.3 H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.2 CH.sub.2 O)                               H    CH(CH.sub.3).sub.2                                                                       H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                            H    CH.sub. 2 CH.sub.3                                                                       H  CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                            H    F         H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                      H    Cl        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     5-Cl Cl        H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    Br        H  OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                          H    NO.sub.2  H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                            H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                     5-OCH.sub.3                                                                         OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                               H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)                 H    SO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7 )                   H    Br        H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             H    NO.sub.2  H  CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                    H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH(CH.sub.3)SCH.sub.2 CH.sub.3                         H    OCH.sub.3 H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                    H    CO.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.2 S)                               __________________________________________________________________________

                                      TABLE 10a                                    __________________________________________________________________________      ##STR117##                                                                    R.sub.17                                                                            R.sub.9 R.sub.21                                                                          X     Y         m.p. (°C.)                              __________________________________________________________________________     H    CH.sub.2 CHCH.sub.2                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                       H    CH.sub.3                                                                               H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                              H    CH.sub.3                                                                               H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCOCH.sub.3                                     H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                            5-F  C.sub.2 H.sub.5                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      4-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OTHP                                            4-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              5-OCH.sub.3                                                                         CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-Cl CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              5-Cl CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OTHP                                            H     .sub.-i-C.sub.3 H.sub.7                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 OCH.sub.3                                                            CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OH                                              H    (CH.sub.2).sub.3 CH.sub.3                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 Cl                                                                   H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                              H     -n-C.sub.3 H.sub.7                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                              H    C.sub.2 H.sub.5                                                                        H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5 ).sub.2                              H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                               H    CH.sub.3                                                                               H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                             H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                                      __________________________________________________________________________

                                      TABLE 10b                                    __________________________________________________________________________      ##STR118##                                                                    R.sub.17                                                                            R.sub.9 R.sub.21                                                                          X     Y          m.p. (°C.)                             __________________________________________________________________________     H    CH.sub.2 CHCH.sub.2                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               CH.sub.3                                                                          CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                       H    CH.sub.3                                                                               H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                              H    CH.sub.3                                                                               H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCOCH.sub.3                                     H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                            5-F  C.sub.2 H.sub.5                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      4-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OTHP                                            4-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              5-OCH.sub.3                                                                         CH.sub. 3                                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-Cl CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              5-Cl CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OTHP                                            H     .sub.-i-C.sub.3 H.sub.7                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 OCH.sub.3                                                            H  CH.sub.3                                                                             CH.sub.2 OH                                              H    (CH.sub.2).sub.3 CH.sub.3                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 Cl                                                                   H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                              H     -n-C.sub.3 H.sub.7                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                              H    C.sub.2 H.sub.5                                                                        H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub. 2                              H    CH.sub.2 CH.sub.3                                                                      H  CH.sub.3                                                                             CH(SCH.sub.2 CH.sub.3).sub.2                             H    CH.sub.3                                                                               H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                        H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                               __________________________________________________________________________

                                      TABLE 10c                                    __________________________________________________________________________      ##STR119##                                                                    R.sub.17                                                                            R.sub.9 R.sub.21                                                                          X     Y            m.p. (°C.)                           __________________________________________________________________________     H    CH.sub.2 CHCH.sub.2                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                       H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                            2-F  C.sub.2 H.sub.5                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      5-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OTHP                                            5-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              2-OCH.sub.3                                                                         CH.sub.3                                                                               H  CH.sub. 3                                                                            CH(OCH.sub.3).sub.2                                      2-Cl CH.sub.3                                                                               H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OH                                              2-Cl CH.sub.3                                                                               H  CH.sub.2 CH.sub.3                                                                    CH(OC.sub.2 H.sub.5).sub.2                               5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OTHP                                            H     .sub.-i-C.sub.3 H.sub.7                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 OCH.sub.3                                                            CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OH                                              H    (CH.sub.2).sub.3 CH.sub.3                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 Cl                                                                   H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                              H     -n-C.sub.3 H.sub.7                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                              H    C.sub.2 H.sub.5                                                                        H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5 ).sub.2                              H    CH.sub.2 CH.sub.3                                                                      H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                               H    CH.sub.3                                                                               CH.sub.3                                                                          OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                             H    CH.sub.3                                                                               H  OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.2 CH.sub.2 O)               __________________________________________________________________________

                                      TABLE 10d                                    __________________________________________________________________________      ##STR120##                                                                    R.sub.17                                                                            R.sub.9 R.sub.21                                                                          X     Y         m.p. (°C.)                              __________________________________________________________________________     H    CH.sub.2 CHCH.sub.2                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                       H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                            5-F  C.sub.2 H.sub.5                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      4-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OTHP                                            4-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              5-OCH.sub.3                                                                         CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-Cl CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              5-Cl CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OTHP                                            H     .sub.-i-C.sub.3 H.sub.7                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 OCH.sub.3                                                            H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                              H    (CH.sub.2).sub.3 CH.sub.3                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 Cl                                                                   H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                              H     -n-C.sub.3 H.sub.7                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                              H    C.sub.2 H.sub.5                                                                        H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub. 2 CH.sub.3                                                                  CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.2 CH.sub.3                                                                      H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.3).sub.2                             H    CH.sub.3                                                                               H  OC.sub.2 H.sub.5                                                                     CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                      H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH(CH.sub.3)(SCH.sub.3)                                  __________________________________________________________________________

                  TABLE 10e                                                        ______________________________________                                          ##STR121##                                                                                                            m.p.                                   R.sub.17                                                                              R.sub.9     R.sub.21 X  Y        (°C.)                           ______________________________________                                         H      CH.sub.2 CHCH.sub.2                                                                        HCH.sub.3   CH(OCH.sub.3).sub.2                             H      CH.sub.3    CH.sub.3 CH.sub.3                                                                          CH(OC.sub.2 H.sub.5).sub.2                      H      CH.sub.3    CH.sub.3 OCH.sub.3                                                                         CH.sub.2 SCH.sub.3                              H      CH.sub.3    HCH.sub.3   CH.sub.2 OH                                     H      CH.sub.3    HOCH.sub.3  CH.sub.2 OCOCH.sub.3                            H      CH.sub.3    HCH.sub.3   CH.sub.2 OCONHC.sub.2 H.sub.5                   5-F    C.sub.2 H.sub.5                                                                            HOCH.sub.3  CH(OCH.sub.3).sub.2                             4-Br   CH.sub.3    HOCH.sub.3  CH.sub. 2 OTHP                                  4-Br   CH.sub.3    HOCH.sub.3  CH.sub.2 OH                                     5-OCH.sub.3                                                                           CH.sub.3    HCH.sub.3   CH(OCH.sub.3).sub.2                             5-Cl   CH.sub.3    HOCH.sub.3  CH.sub.2 OH                                     5-Cl   CH.sub.3    HCH.sub.3   CH(OC.sub.2 H.sub.5).sub.2                      5-CH.sub.3                                                                            CH.sub.3    HCH.sub.2 CH.sub.3                                                                         CH(OCH.sub.3).sub.2                             5-CH.sub.3                                                                            CH.sub.3    HCH.sub.3   CH.sub.2 OTHP                                   H       .sub.-i-C.sub.3 H.sub.7                                                                   HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                     H      CH.sub.2 CH.sub.2 OCH.sub.3                                                                HCH.sub.3   CH.sub.2 OH                                     H      (CH.sub.2).sub.3 CH.sub.3                                                                  HCH.sub.3   CH(OCH.sub.3).sub.2                             H      CH.sub.3    HOCH.sub.3  CH(OCH.sub.3).sub.2                             H      CH.sub.3    HOCH.sub.3  CH.sub.2 OH                                     H      CH.sub.2 CH.sub.2 Cl                                                                       HCH.sub.3   CH.sub.2 OH                                     H      CH.sub.3    HCH.sub.3   CH.sub.2 OCOC.sub.2 H.sub.5                     H       -n-C.sub.3 H.sub.7                                                                        HCH.sub.3   CH(OCH.sub.3).sub.2                             H      CH.sub.3    HOCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                        H      CH.sub.3    HCH.sub.3   CH.sub.2 OCO.sub.2 CH.sub.3                     H      C.sub.2 H.sub.5                                                                            HCH.sub. 3  CH(OCH.sub.3).sub.2                             H      CH.sub.3    HOCH.sub.3  CH(OC.sub.2 H.sub.5).sub.2                      H      CH.sub.3    HCH.sub.3   CH.sub.2 SCH.sub.2 CH.sub.3                     H      CH.sub.3    HOCH.sub.3  CH(CH.sub.3)SCH.sub.3                           H      CH.sub.3    HCH.sub.3   CH.sub.2 SO.sub.2 CH.sub.3                      ______________________________________                                    

                  TABLE 10f                                                        ______________________________________                                          ##STR122##                                                                                                      m.p.                                         R.sub.17 R.sub.9                                                                             R.sub.21 XY         (°C.)                                 ______________________________________                                         HCH.sub.2 CHCH.sub.2                                                                         HCH.sub.3 CH(OCH.sub.3).sub.2                                    HCH.sub.3     HCH.sub.2 CH.sub.3 CH(OC.sub.2 H.sub.5).sub.2                    HCH.sub.3     HOCH.sub.2 CH.sub.3 CH.sub.2 SCH.sub.3                           HCH.sub.3     HCH.sub.3 CH.sub.2 OH                                            HCH.sub.3     HOCH.sub.3 CH.sub.2 OCOCH.sub.3                                  HCH.sub.3     HCH.sub.3 CH.sub.2 OCONHC.sub.2 H.sub.5                          2-FC.sub.2 H.sub.5                                                                           HOCH.sub.3 CH(OCH.sub.3).sub.2                                   5-BrCH.sub.3  H OCH.sub.3 CH.sub.2 OTHP                                        5-BrCH.sub.3  HOCH.sub.3 CH.sub.2 OH                                           2-OCH.sub.3 CH.sub.3                                                                         HCH.sub.3 CH(OCH.sub.3).sub.2                                    2-ClCH.sub.3  HOCH.sub.3 CH.sub.2 OH                                           2-ClCH.sub.3  CH.sub.3 CH.sub.3 CH(OC.sub.2 H.sub.5).sub.2                     5-CH.sub.3 CH.sub.3                                                                          HCH.sub.3 CH(OCH.sub.3).sub.2                                    5-CH.sub.3 CH.sub.3                                                                          HCH.sub.3 CH.sub.2 OTHP                                          H .sub.-i-C.sub.3 H.sub.7                                                                    HOCH.sub.3 CH.sub.2 OH                                           HCH.sub.2 CH.sub.2 OCH.sub.3                                                                 HCH.sub.3 CH.sub.2 OH                                            H(CH.sub.2).sub.3 CH.sub.3                                                                   HCH.sub.3 CH(OCH.sub.3).sub.2                                    HCH.sub.3     HOCH.sub.3 CH(OCH.sub.3).sub.2                                   HCH.sub.3     HOCH.sub.3 CH.sub.2 OH                                           HCH.sub.2 CH.sub.2 Cl                                                                        HCH.sub.3 CH.sub.2 OH                                            HCH.sub.3     HCH.sub.3 CH.sub.2 OCOC.sub.2 H.sub.5                            H -n-C.sub.3 H.sub.7                                                                         HCH.sub.3 CH(OCH.sub.3).sub.2                                    HCH.sub.3     HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                              HCH.sub.3     HCH.sub.3 CH.sub.2 OCO.sub.2 CH.sub.3                            HC.sub.2 H.sub.5                                                                             HCH.sub.3 CH(OCH.sub.3).sub.2                                    HCH.sub.3     HOCH.sub.3 CH(OC.sub.2 H.sub.5).sub.2                            HCH.sub.3     HOCH.sub.3 CH(SCH.sub.2 CH.sub.2 S)                              HCH.sub.3     HOCH.sub.3 CH(OCH(CH.sub.3)CH.sub.2 O)                           HCH.sub.3     HOCH.sub.3 C(CH.sub.3)(OCH.sub.3).sub.2                          ______________________________________                                    

                  TABLE 11a                                                        ______________________________________                                          ##STR123##                                                                    R.sub.18                                                                             R.sub.21                                                                              X          Y             m.p.(°C.)                         ______________________________________                                         H     H      CH.sub.3   CH(OCH.sub.3).sub.2                                    H     H      CH.sub.3   CH.sub.2 OTHP                                          H     H      OCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                            H     H      OCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                               Cl    H      CH.sub.3   CH(OCH.sub.3).sub.2                                    Cl    H      CH.sub.2 CH.sub.3                                                                         CH(OC.sub.2 H.sub.5).sub.2                             Cl    H      CH.sub.3   CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 OTHP                                          Cl    CH.sub.3                                                                              OCH.sub.3  CH(OCH.sub.3).sub.2                                    Cl    H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   Cl    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      CH.sub.3   CH(OCH.sub.3).sub.2                                    Br    H      CH.sub.3   CH(OC.sub.2 H.sub.5).sub.2                             Br    H      CH.sub. 3  CH.sub.2 OH                                            Br    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      OCH.sub.3  CH.sub.2 OCO.sub.2 CH.sub.3                            CH.sub.3                                                                             H      CH.sub.3   CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      CH.sub.3   CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OH                                            CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OCONHC.sub.2 H.sub.5                          CH.sub.3                                                                             H      OCH.sub.3  CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OTHP                                          CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 SO.sub.2 CH.sub.3                             Br    H      OCH.sub.3  CH(SCH.sub.3).sub.2                                    CH.sub.3                                                                             H      OCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                           ______________________________________                                    

                  TABLE 11b                                                        ______________________________________                                          ##STR124##                                                                    R.sub.18                                                                             R.sub.21                                                                              X          Y             m.p.(°C.)                         ______________________________________                                         H     H      CH.sub.3   CH(OCH.sub.3).sub.2                                    H     H      CH.sub.3   CH.sub.2 OTHP                                          H     H      OCH.sub.3  CH.sub.2 OH                                            H     H      OCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                               Cl    H      CH.sub.2 CH.sub.3                                                                         CH(OCH.sub.3).sub.2                                    Cl    H      CH.sub.3   CH(OC.sub.2 H.sub.5).sub.2                             Cl    CH.sub.3                                                                              CH.sub.3   CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 OTHP                                          Cl    H      OCH.sub.3  CH(OCH.sub.3).sub.2                                    Cl    H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   Cl    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      CH.sub.3   CH(OCH.sub.3).sub.2                                    Br    H      CH.sub.3   CH(OC.sub.2 H.sub.5 ).sub.2                            Br    H      CH.sub.3   CH.sub.2 OH                                            Br    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      OCH.sub.2 CH.sub.3                                                                        CH.sub.2 OCO.sub.2 CH.sub.3                            CH.sub.3                                                                             H      CH.sub.3   CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      CH.sub.3   CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                      CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OH                                            CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OCONHC.sub.2 H.sub.5                          CH.sub.3                                                                             H      OCH.sub.3  CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OTHP                                          CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 SO.sub.2 CH.sub.3                             Br    H      CH.sub.3   CH(SCH.sub.3).sub.2                                    CH.sub.3                                                                             H      CH.sub.3   CH(SCH.sub.2 CH.sub.3).sub.2                           ______________________________________                                    

                  TABLE 12                                                         ______________________________________                                          ##STR125##                                                                                                     m.p.                                          R.sub.19     R.sub.21 XY         Z (°C.)                                ______________________________________                                         Cl           HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           Cl           CH.sub.3 CH.sub.3 CH.sub.2 OCOCH.sub.3                                                              CH                                           Cl           HCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                  N                                            Cl           HOCH.sub.3 CH.sub.2 SCH.sub.3                                                                       N                                            Cl           HOCH.sub.3 CH(OEt).sub.2                                                                            CH                                           NO.sub.2     HC.sub.2 H.sub.5 CH(SCH.sub.2 CH.sub.2 S)                                                           CH                                           NO.sub.2     HCH.sub.3 CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                         CH                                           NO.sub.2     HClCH(OCH.sub.3).sub.2                                                                              CH                                           NO.sub.2     HCH.sub.3 CH(OCH(CH.sub.3)CH.sub.2 O)                                                               N                                            NO.sub.2     HOCH.sub.3 CH.sub.2 SEt                                                                             CH                                           NO.sub.2     HOCH.sub.3 CH.sub.2 OH                                                                              CH                                           CF.sub.3     HOC.sub.2 H.sub.5 CH.sub.2 OTHP                                                                     CH                                           CF.sub.3     HCH.sub.3 CH.sub.2 OCON(CH.sub.3).sub.2                                                             CH                                           CF.sub.3     HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           CF.sub.3     HCH.sub.3 CH(OEt).sub.2                                                                             N                                            CF.sub.3     HOCH.sub.3 CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                        CH                                           OCH.sub.3    CH.sub.3 OCH.sub.3 CH(OCH(CH.sub.3)CH.sub.2 O)                                                      CH                                           OCH.sub.3    HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                 CH                                           OCH.sub.3    HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                      CH                                           OCH.sub.3    HCH.sub.3 CH(OEt).sub.2                                                                             N                                            OCH.sub.3    HCH.sub.3 CH.sub.2 SCH.sub.3                                                                        CH                                           OCH.sub.3    HCH.sub.3 CH.sub.2 SEt                                                                              CH                                           OCH.sub.3    HCH.sub.3 CH.sub.2 OCONHCH.sub.3                                                                    CH                                           CO.sub.2 CH.sub.3                                                                           HCH.sub.3 CH.sub.2 SEt                                                                              CH                                           CO.sub.2 CH.sub.3                                                                           CH.sub.3 CH.sub.3 CH(OEt).sub.2                                                                     N                                            CO.sub.2 CH.sub.3                                                                           CH.sub.3 CH.sub.3 CH(SCH.sub.2 CH.sub.2 S)                                                          CH                                           Cl           HOCH.sub.3 CH(SCH.sub.3).sub.2                                                                      CH                                           NO.sub.2     HCH.sub.3 CH.sub.2 SO.sub.2 CH.sub.3                                                                CH                                           CO.sub.2 CH.sub.3                                                                           HOCH.sub.3 C(CH.sub.3)(OCH.sub.3).sub.2                                                             CH                                           CO.sub.2 CH.sub.3                                                                           CH.sub.3 OCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                         CH                                           CO.sub.2 CH.sub.3                                                                           CH.sub.3 OCH.sub.3 CH(OCH.sub.3).sub.2                                                              CH                                           CO.sub.2 CH.sub.3                                                                           CH.sub.3 OCH.sub.3 CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                N                                            CO.sub.2 CH.sub.2 CH.sub.3                                                                  CH.sub.3 C.sub.2 H.sub.5 CH(OCH.sub.3).sub.2                                                        CH                                           CO.sub.2 CH.sub.2 CH.sub.3                                                                  CH.sub.3 OC.sub.2 H.sub.5 CH(OCH.sub.3).sub.2                                                       CH                                           CO.sub.2 CH.sub.2 CH.sub.3                                                                  CH.sub.3 OCH.sub.3 CH(OCH.sub.3).sub.2                                                              CH                                           CO.sub.2 -n-C.sub.4 H.sub.9                                                                 CH.sub.3 OCH.sub.3 CH.sub.2 OH                                                                      CH                                           CO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                            CH.sub.3 OCH.sub.3 CH.sub.2 OH                                                                      N                                            SO.sub.2 N(OCH.sub.3)CH.sub.3                                                               CH.sub.3 OCH.sub.3 CH.sub.2 OH                                                                      CH                                           SO.sub.2 N(CH.sub.3).sub.2                                                                  HCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                  CH                                           SO.sub.2 N(CH.sub.3).sub.2                                                                  CH.sub.3 CH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                                                         CH                                           SO.sub.2 N(CH.sub.3).sub.2                                                                  HCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                  N                                            SO.sub.2 N(CH.sub.3).sub.2                                                                  HCH.sub.3 CH.sub.2 OCOCH.sub.3                                                                      CH                                           SO.sub.2 N(CH.sub.3).sub.2                                                                  HOCH.sub.3 CH.sub.2 OCO.sub.2 CH.sub.3                                                              CH                                           SO.sub.2 N(CH.sub.3).sub.2                                                                  HOCH.sub.3 CH.sub.2 SCH.sub.3                                                                       CH                                           SO.sub.2 N(CH.sub.3).sub.2                                                                  HOCH.sub.3 CH.sub.2 OTHP                                                                            CH                                           SO.sub.2 (CH.sub.2 CH.sub.3)CH.sub.3                                                        HOCH.sub.3 CH.sub.2 OH                                                                              N                                            SO.sub.2 (CH.sub.2 CH.sub.3)CH.sub.3                                                        HCH.sub.3 CH.sub.2 OH                                                                               CH                                           OSO.sub.2 CH.sub.3                                                                          HCH.sub.3 CH.sub.2 OH                                                                               CH                                           OSO.sub.2 CH.sub.3                                                                          HCH.sub.3 CH(OCH.sub.2 CH.sub.3).sub.2                                                              CH                                           OSO.sub.2 CH.sub.3                                                                          HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           OSO.sub.2 CH.sub.3                                                                          HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                      CH                                           OSO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                      N                                            OSO.sub.2 CH.sub.2 CF.sub.3                                                                 HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                 CH                                           SCH.sub.3    HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           SCH.sub.3    CH.sub.3 CH.sub.3 CH.sub.2 OCOC.sub.2 H.sub.5                                                       N                                            SCH.sub.3    HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                                 N                                            SCH.sub.2 CH.sub.3                                                                          HOCH.sub.3 CH.sub.2 SCH.sub.3                                                                       CH                                           SCH.sub.2 CH.sub.3                                                                          HClCH(OEt).sub.2     CH                                           SO.sub.2 CH.sub.3                                                                           CH.sub.3 OCH.sub.3 CH(SCH.sub.2 CH.sub.2 S)                                                         N                                            SO.sub.2 CH.sub.3                                                                           HCH.sub.3 CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                         CH                                           SO.sub.2 CH.sub.3                                                                           HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                                 HC.sub.2 H.sub.5 CH(OCH(CH.sub.3)CH.sub.2 O)                                                        CH                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                                 HOCH.sub.3 CH.sub.2 SEt                                                                             N                                            SO.sub.2 -n-C.sub.3 H.sub.7                                                                 HOCH.sub.3 CH.sub.2 OH                                                                              CH                                           SO.sub.2 CH.sub.2 CHCH.sub.2                                                                HOCH.sub.3 CH.sub.2 OTHP                                                                            CH                                           SO.sub.2 -n-C.sub.4 H.sub.9                                                                 HOCH.sub.3 CH.sub.2 OH                                                                              CH                                           S  .sub.-t-C.sub.4 H.sub.9                                                                  HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           OCH.sub.2 CH.sub.2 Cl                                                                       HCH.sub.3 CH.sub.2 OCON(CH.sub.3).sub.2                                                             CH                                           OCHFCHF.sub.2                                                                               HOC.sub.2 H.sub.5 CH.sub.2 OCO.sub.2 Et                                                             N                                            OCH.sub.2 CF.sub.3                                                                          HOCH.sub.3 CH.sub.2 OCO.sub.2 CH.sub.3                                                              CH                                           O -n-C.sub.3 H.sub.7                                                                        HOCH.sub.3 CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                        CH                                           O -n-C.sub.3 H.sub.7                                                                        HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                        CH                                           O -n-C.sub.3 H.sub.7                                                                        HClCH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                                CH                                           O -n-C.sub.4 H.sub.9                                                                        HOCH.sub.3 CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                        N                                            O -n-C.sub.4 H.sub.9                                                                        HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           OCH.sub.2 CH.sub.3                                                                          HCH.sub.3 CH(OCH.sub.2 CH.sub.3).sub.2                                                              CH                                           OCH.sub.2 CH.sub.3                                                                          HCH.sub.3 CH.sub.2 OH                                                                               CH                                           OCF.sub.3    CH.sub.3 OCH.sub.3 CH(OCH.sub.2 CH.sub.2 O)                                                         CH                                           OCF.sub.3    HOCH.sub.3 CH.sub.2 SCH.sub.3                                                                       N                                            OCF.sub.3    HOCH.sub.3 CH.sub.2 OH                                                                              CH                                           CH.sub.2 Cl  HCH.sub.3 CH(OCH.sub.3).sub.2                                                                       CH                                           CH.sub.2 Cl  HOCH.sub.3 CH(OCH.sub.3).sub.2                                                                      N                                            ______________________________________                                    

                                      TABLE 13                                     __________________________________________________________________________      ##STR126##                                                                    R.sub.19   R.sub.20                                                                            R.sub.21                                                                          X   Y           Z  m.p.(°C.)                         __________________________________________________________________________                Cl   H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                                     Cl   CH.sub.3                                                                          CH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                                                       CH                                                     Cl   H  CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   N                                                      Cl   H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         N                                                      Cl   H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              CH                                                     NO.sub.2                                                                            H  C.sub.2 H.sub.5                                                                    CH(SCH.sub.2 CH.sub.2 S)                                                                   CH                                                     NO.sub.2                                                                            H  CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                                     NO.sub.2                                                                            H  Cl  CH(OCH.sub.3).sub.2                                                                        CH                                                     NO.sub.2                                                                            H  CH.sub.3                                                                           CH(OCH(CH.sub.3)CH.sub.2 O)                                                                N                                                      NO.sub.2                                                                            H  OCH.sub.3                                                                          CH.sub.2 SEt                                                                               CH                                                     NO.sub.2                                                                            H  OCH.sub.3                                                                          CH.sub.2 OH CH                                                     CF.sub.3                                                                            H  OC.sub.2 H.sub.5                                                                   CH.sub.2 OTHP                                                                              CH                                                     CF.sub.3                                                                            H  CH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                                                              CH                                                     CF.sub.3                                                                            H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                                     CF.sub.3                                                                            H  CH.sub.3                                                                           CH(OEt).sub.2                                                                              N                                                      CF.sub.3                                                                            H  OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                          CH                                                     OCH.sub.3                                                                           CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                                                                CH                                                     OCH.sub.3                                                                           H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                                     OCH.sub.3                                                                           H  OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                                     OCH.sub.3                                                                           H  CH.sub.3                                                                           CH(OEt).sub.2                                                                              N                                                      OCH.sub.3                                                                           H  CH.sub.3                                                                           CH.sub.2 SCH.sub.3                                                                         CH                                                     OCH.sub.3                                                                           H  CH.sub.3                                                                           CH.sub.2 SEt                                                                               CH                                                     OCH.sub.3                                                                           H  CH.sub.3                                                                           CH.sub.2 OCONHCH.sub.3                                                                     CH                                                     CO.sub.2 CH.sub.3                                                                   H  CH.sub.3                                                                           CH.sub.2 SEt                                                                               CH                                                     CO.sub.2 CH.sub.3                                                                   CH.sub.3                                                                          CH.sub.3                                                                           CH(OEt).sub.2                                                                              N                                                      CO.sub.2 CH.sub.3                                                                   CH.sub.3                                                                          CH.sub.3                                                                           CH(SCH.sub.2 CH.sub.2 S)                                                                   CH                                          CO.sub.2 CH.sub.3                                                                              CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                          CO.sub.2 CH.sub.3                                                                              CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.3 ).sub.2                                                                       CH                                          CO.sub.2 CH.sub.3                                                                              CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          N                                           CO.sub.2 CH.sub.2 CH.sub.3                                                                     CH.sub.3                                                                          C.sub.2 H.sub.5                                                                    CH(OCH.sub.3).sub.2                                                                        CH                                          CO.sub.2 CH.sub.2 CH.sub.3                                                                     CH.sub.3                                                                          OC.sub.2 H.sub.5                                                                   CH(OCH.sub.3).sub.2                                                                        CH                                          CO.sub.2 CH.sub.2 CH.sub.3                                                                     CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                          CO.sub.2 -n-C.sub.4 H.sub.9                                                                    CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OH CH                                          CO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                               CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OH N                                           SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                  CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OH CH                                          SO.sub.2 N(CH.sub.3).sub.2                                                                     H  CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                          SO.sub.2 N(CH.sub.3).sub.2                                                                     CH.sub.3                                                                          CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                          SO.sub.2 N(CH.sub.3).sub.2                                                                     H  CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   N                                           SO.sub.2 N(CH.sub.3).sub.2                                                                     H  CH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                                                       CH                                          SO.sub.2 N(CH.sub.3).sub.2                                                                     H  OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                                                                CH                                          SO.sub.2 N(CH.sub.3).sub.2                                                                     H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         CH                                          SO.sub.2 N(CH.sub.3).sub.2                                                                     H  OCH.sub.3                                                                          CH.sub.2 OTHP                                                                              CH                                          OSO.sub.2 CH.sub.3                                                                             H  CH.sub.3                                                                           CH.sub.2 OH CH                                          OSO.sub.2 CH.sub.3                                                                             H  CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.3).sub.2                                                               CH                                          OSO.sub.2 CH.sub.3                                                                             H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                          OSO.sub.2 CH.sub.3                                                                             H  OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                          OSO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                          H  OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        N                                           OSO.sub.2 CH.sub.2 CF.sub.3                                                                    H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                          CH.sub.3        H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                          CH.sub.3        CH.sub.3                                                                          CH.sub.3                                                                           CH.sub.2 OCOC.sub.2 H.sub.5                                                                N                                           CH.sub.3        H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   N                                           CH.sub.2 CH.sub.3                                                                              H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         CH                                          CH.sub.2 CH.sub.3                                                                              H  Cl  CH(OEt).sub.2                                                                              CH                                          CH.sub.3        H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                           -n-C.sub.3 H.sub. 7                                                                           H  C.sub.2 H.sub.5                                                                    CH(OCH(CH.sub.3)CH.sub.2 O)                                                                CH                                           -n-C.sub.3 H.sub.7                                                                            H  OCH.sub.3                                                                          CH.sub.2 SEt                                                                               N                                            -n-C.sub.3 H.sub.7                                                                            H  OCH.sub.3                                                                          CH.sub.2 OH CH                                           -n-C.sub.4 H.sub.9                                                                            H  OCH.sub.3                                                                          CH.sub.2 OH CH                                          C.sub.4 H.sub.9 H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                          OCH.sub.2 CH.sub.2 Cl                                                                          H  CH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                                                              CH                                          OCHFCHF.sub.2   H  OC.sub.2 H.sub.5                                                                   CH.sub.2 OCO.sub.2 Et                                                                      N                                           OCH.sub.2 CF.sub.3                                                                             H  OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                                                                CH                                          O -n-C.sub.3 H.sub.7                                                                           H  OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                          CH                                          O -n-C.sub.3 H.sub.7                                                                           H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                          O -n-C.sub.3 H.sub.7                                                                           H  Cl  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                          O -n-C.sub.4 H.sub.9                                                                           H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          N                                           O -n-C.sub.4 H.sub.9                                                                           H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                          OCH.sub.2 CH.sub.3                                                                             H  CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.3).sub.2                                                               CH                                          OCH.sub.2 CH.sub.3                                                                             H  CH.sub.3                                                                           CH.sub.2 OH CH                                          OCF.sub.3       CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                          OCF.sub.3       H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         N                                           OCF.sub.3       H  OCH.sub.3                                                                          CH.sub.2 OH CH                                          CH.sub.2 Cl     H  CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                          CH.sub.2 Cl     H  OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                          __________________________________________________________________________

Formulations

Useful formulations of the compounds of Formula I can be prepared in conventional ways. They include dusts, granules, pellets, solutions, suspensions, emulsions, wettable powders, emulsifiable concentrates and the like. Many of these may be applied directly. Sprayable formulations can be extended in suitable media and used at spray volumes of from a few liters to several hundred liters per hectare. High strength compositions are primarily used as intermediates for further formulation. The formulations, broadly, can contain from about 0.1% to 99% by weight of active ingredient(s) and at least one of (a) about 0.1% to 20% surfactant(s) and (b) about 1% to 99.9% solid or liquid inert diluent(s). More specifically, they will contain these ingredients in the following approximate proportions:

                  TABLE 14                                                         ______________________________________                                                     Active  Weight Percent*                                                        Ingredient                                                                             Diluent(s)                                                                               Surfactant(s)                                    ______________________________________                                         Wettable Powders                                                                             20-90      0-74     1-10                                         Oil Suspensions,                                                                              3-50     40-95     0-15                                         Emulsions, Solutions,                                                          (including Emulsifiable                                                        Concentrates)                                                                  Aqueous Suspension                                                                           10-50     40-84     1-20                                         Dusts          1-25     70-99     0-5                                          Granules and Pellets                                                                         0.1-95      5-99.9  0-15                                         High Strength 90-99      0-10     0-2                                          Compositions                                                                   ______________________________________                                          *Active ingredient plus at least one of a Surfactant or a Diluent equals       100 weight percent.                                                      

Lower or higher levels of active ingredients can, of course, be present depending on the intended use and the physical properties of the compound. Higher ratios of surfactant to active ingredient are sometimes desirable, and are achieved by incorporation into the formulation or by tank mixing.

Typical solid diluents are described in Watkins, et al., "Handbook of Insecticide Dust Diluents and Carriers", 2nd Ed., Dorland Books, Caldwell, N.J., but other solids, either mined or manufactured, may be used. The more absorptive diluents are preferred for wettable powders and the denser ones for dusts. Typical liquid diluents and solvents are described in Marsden, "Solvents Guide," 2nd Ed., Interscience, New York, 1950. Solubility under 0.1% is preferred for suspension concentrates; solution concentrates are preferably stable against phase separation at 0° C. "McCutcheon's Detergents and Emulsifiers Annual", MC Publishing Corp., Ridgewood, N.J., as well as Sisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publishing Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foaming, caking, corrosion, microbiological growth, etc.

The methods of making such compositions are well known. Solutions are prepared by simply mixing the ingredients. Fine solid compositions are made by blending and, usually, grinding as in a hammer or fluid energy mill. Suspensions are prepared by wet milling (see, for example, Littler, U.S. Pat. No. 3,060,084). Granules and pellets may be made by spraying the active material upon preformed granular carriers or by agglomeration techniques. See J. E. Browning, "Agglomeration", Chemical Engineering, Dec. 4, 1967, pp. 147ff. and "Perry's Chemical Engineer's Handbook", 5th Ed., McGraw-Hill, New York, 1973, pp. 8-57ff.

For further information regarding the art of formulation, see for example:

H. M. Loux, U.S. Pat. No. 3,235,361, Feb. 15, 1966, Col. 6, line 16 through Col. 7, line 19 and Examples 10 through 41;

R. W. Luckenbaugh, U.S. Pat. No. 3,309,192, Mar. 14, 1967, Col. 5, line 43 through Col. 7, line 62 and Examples 8, 12, 15, 39, 41, 52, 53, 58, 132, 138-140, 162-164, 166, 167 and 169-182;

H. Gysin and E. Knusli, U.S. Pat. No. 2,891,855, June 3, 1959, Col. 3, line 66 through Col. 5, line 17 and Examples 1-4;

G. C. Klingman, "Weed Control as a Science", John Wiley & Sons, Inc., New York, 1961, pp. 81-96; and

J. D. Fryer and S. A. Evans, "Weed Control Handbook", 5th Ed., Blackwell Scientific Publications, Oxford, 1968, pp. 101-103.

In the following examples, all parts are by weight unless otherwise indicated.

EXAMPLE 7 Wettable Powder

    ______________________________________                                          3-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)-                                                          80%                                                 aminocarbonyl]aminosulfonyl]-2-thiophene-                                      carboxylic acid, methyl ester                                                  sodium alkylnaphthalenesulfonate                                                                          2%                                                  sodium ligninsulfonate     2%                                                  synthetic amorphous silica 3%                                                  kaolinite                  13%                                                 ______________________________________                                    

The ingredients are blended, hammer-milled until all the solids are essentially under 50 microns, reblended, and packaged.

EXAMPLE 8 Wettable Powder

    ______________________________________                                         N--[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)-                                                            50%                                                aminocarbonyl]-2-(methylsulfonyl)benzene-                                      sulfonamide                                                                    sodium alkylnaphthalenesulfonate                                                                            2%                                                low viscosity methyl cellulose                                                                              2%                                                diatomaceous earth          46%                                                ______________________________________                                    

The ingredients are blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in diameter. The product is reblended before packaging.

EXAMPLE 9 Granule

    ______________________________________                                         Wettable Powder of Example 8                                                                           5%                                                     attapulgite granules   95%                                                     (U.S.S. 20-40 mesh; 0.84-0.42 mm)                                              ______________________________________                                    

A slurry of wettable powder containing ≈25% solids is sprayed on the surface of attapulgite granules in a double-cone blender. The granules are dried and packaged.

EXAMPLE 10 Extruded Pellet

    ______________________________________                                         N--[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)amino-                                                        25%                                               carbonyl]-2-nitrobenzenesulfonamide                                            anhydrous sodium sulfate     10%                                               crude calcium ligninsulfonate                                                                                5%                                               sodium alkylnaphthalenesulfonate                                                                             1%                                               calcium/magnesium bentonite  59%                                               ______________________________________                                    

The ingredients are blended, hammer-milled and then moistened with about 12% water. The mixture is extruded as cylinders about 3 mm diameter which are cut to produce pellets about 3 mm long. These may be used directly after drying, or the dried pellets may be crushed to pass a U.S.S. No. 20 sieve (0.84 mm openings). The granules held on a U.S.S. No. 40 sieve (0.42 mm openings) may be packaged for use and the fines recycled.

EXAMPLE 11 Oil Suspension

    ______________________________________                                         5-chloro-2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-                                                       25%                                               yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl                            ester                                                                          polyoxyethylene sorbitol hexaoleate                                                                          5%                                               highly aliphatic hydrocarbon oil                                                                            70%                                               ______________________________________                                    

The ingredients are ground together in a sand mill until the solid particles have been reduced to under about 5 microns. The resulting thick suspension may be applied directly, but preferably after being extended with oils or emulsified in water.

EXAMPLE 12 Wettable Powder

    ______________________________________                                         2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl]-                                                         20%                                                  aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          sodium alkylnaphthalenesulfonate                                                                         4%                                                   sodium ligninsulfonate    4%                                                   low viscosity methyl cellulose                                                                           3%                                                   attapulgite               69%                                                  ______________________________________                                    

The ingredients are thoroughly blended. After grinding in a hammer-mill to produce particles essentially all below 100 microns, the material is reblended and sifted through a U.S.S. No. 50 sieve (0.3 mm openings) and packaged.

EXAMPLE 13 Low Strength Granule

    ______________________________________                                         2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)-                                                          1%                                                  pyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-                                   benzoic acid, methyl ester                                                     N,N--dimethylformamide     9%                                                  attapulgite granules       90%                                                 (U.S.S. 20-40 sieve)                                                           ______________________________________                                    

The active ingredient is dissolved in the solvent and the solution is sprayed upon dedusted granules in a double cone blender. After spraying of the solution has been completed, the blender is allowed to run for a short period and then the granules are packaged.

EXAMPLE 14 Aqueous Suspension

    ______________________________________                                         2-[[[4-(acetyloxymethyl)-6-methylpyrimidin-2-yl]-                                                         40%                                                 aminocarbonyl]aminosulfonyl]benzoic acid,                                      methyl ester                                                                   polyacrylic acid thickener 0.3%                                                dodecylphenol polyethylene glycol ether                                                                   0.5%                                                disodium phosphate         1%                                                  monosodium phosphate       0.5%                                                polyvinyl alcohol          1.0%                                                water                      56.7%                                               ______________________________________                                    

The ingredients are blended and ground together in a sand mill to produce particles essentially all under 5 microns in size.

EXAMPLE 15 Solution

    ______________________________________                                         5-chloro-2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-                                                         5%                                               yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl                            ester, sodium salt                                                             water                        95%                                               ______________________________________                                    

The salt is added directly to the water with stirring to produce the solution, which may then be

EXAMPLE 16 Low Strength Granule

    ______________________________________                                         2-[[[4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]-                                                         0.1%                                                aminocarbonyl]aminosulfonyl]benzoic acid,                                      methyl ester                                                                   attapulgite granules      99.9%                                                (U.S.S. 20-40 mesh)                                                            ______________________________________                                    

The active ingredient is dissolved in a solvent and the solution is sprayed upon dedusted granules in a double-cone blender. After spraying of the solution has been completed, the material is warmed to evaporate the solvent. The material is allowed to cool and then packaged.

EXAMPLE 17 Granule

    ______________________________________                                         2-[ [(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)-                                                        80%                                                aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          wetting agent                1%                                                crude ligninsulfonate salt (containing                                                                     10%                                                5-20% of the natural sugars)                                                   attapulgite clay             9%                                                ______________________________________                                    

The ingredients are blended and milled to pass through a 100 mesh screen. This material is then added to a fluid bed granulator, the air flow is adjusted to gently fluidize the material, and a fine spray of water is sprayed onto the fluidized material. The fluidization and spraying are continued until granules of the desired size range are made. The spraying is stopped, but fluidization is continued, optionally with heat, until the water content is reduced to the desired level, generally less than 1%. The material is then discharged, screened to the desired size range, generally 14-100 mesh (1410-149 microns), and packaged for use.

EXAMPLE 18 High Strength Concentrate

    ______________________________________                                         2-[[(4-(1,3-dioxolan-2-yl)-6-methoxypyrimidin-2-yl)-                                                        99%                                               aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          silica aerogel              0.5%                                               synthetic amorphous silica  0.5%                                               ______________________________________                                    

The ingredients are blended and ground in a hammer-mill to produce a material essentially all passing a U.S.S. No. 50 screen (0.3 mm opening). The concentrate may be formulated further if necessary.

EXAMPLE 19 Wettable Powder

    ______________________________________                                         2-[[(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)-                                                          90%                                               aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          dioctyl sodium sulfosuccinate                                                                              0.1%                                               synthetic fine silica       9.9%                                               ______________________________________                                    

The ingredients are blended and ground in a hammer-mill to produce particles essentially all below 100 microns. The material is sifted through a U.S.S. No. 50 screen and then packaged.

EXAMPLE 20 Wettable Powder

    ______________________________________                                         2-chloro-N--[[4-(dimethoxymethyl)-6-methylpyrimidin-                                                        40%                                               2-yl]aminocarbonyl]benzenesulfonamide                                          sodium ligninsulfonate       20%                                               montmorillonite clay         40%                                               ______________________________________                                    

The ingredients are thoroughly blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in size. The material is reblended and then packaged.

EXAMPLE 21 Oil Suspension

    ______________________________________                                         2-[[[4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]amino-                                                      35%                                               carbonyl]aminosulfonyl]benzoic acid,                                           2-propyl ester                                                                 blend of polyalcohol carboxylic                                                                              6%                                               esters and oil soluble petroleum                                               sulfonates                                                                     xylene                       59%                                               ______________________________________                                    

The ingredients are combined and ground together in a sand mill to produce particles essentially all below 5 microns. The product can be used directly, extended with oils, or emulsified in water.

Utility

The compounds of the present invention are highly active herbicides. They have utility for broad-spectrum pre- and/or post-emergence weed control in areas where complete control of all vegetation is desired, such as around fuel storage tanks, ammunition depots, industrial storage areas, parking lots, drive-in theaters, around billboards, highway and railroad structures. Alternatively, the subject compounds are useful for selective pre- or post-emergence weed control in crops, such as cotton, soybeans and wheat.

The rates of application for the compounds of the invention are influenced by a number of factors, including their use whether as selective or general herbicides, the crop species involved, the types of weeds to be controlled, weather and climate, formulation ingredients, mode of application, amount of foliage present, etc. In general terms, the subject compounds should be applied at levels of around 0.01 to 5 kg/ha, the lower rates being suggested for use on lighter soils and/or those having a low organic matter content, for selective weed control or for situations where only short-term persistence is required.

The compounds of the invention may be used in combination with any other commerical herbicide, such as, for example those listed below.

The compounds of this invention may be used in combination with other commercial herbicides such as:

    ______________________________________                                         Common                                                                         Name     Chemical Name                                                         ______________________________________                                         acifluorfen                                                                             5-[2-chloro-4-(trifluoromethyl)phenoxy]-                                       2-nitrobenzoic acid                                                   alachlor 2-chloro-2',6'-diethyl-N--(methoxymethyl)-                                     acetanilide                                                           amitrole 3-amino- .sub.-s-triazole                                             atrazine 2-chloro-4-(ethylamino)-6-(isopropyl-                                          amino)- .sub.-s-triazine                                              barban   4-chloro-2-butynyl  .sub.--m-chlorocarbanilate                        bentazon 3-isopropyl-1H--2,1,3-benzothiadiazin-                                         4(3H)--one 2,2-dioxide                                                benzoylprop                                                                             N--benzoyl-N--(3,4-dichlorophenyl)-DL-                                         alaine                                                                bromacil 5-bromo-3-sec-butyl-6-methyluracil                                    bromoxynil                                                                              3,5-dibromo-4-hydroxybenzonitrile                                     butylate S--ethyl-diisobutylthiocarbamate                                      CGA 82725                                                                               2-(4-(3,5-dichloropyridin-2-yloxy)phen-                                        oxy-propanoic acid, propynyl ester                                    chlortoluron                                                                            N'--(3-chloro-4-methylphenyl-N',N'--                                           dimethylurea                                                          cyanazine                                                                               2-[[4-chloro-6-(ethylamino)- .sub.-s-triazin-                                  2-yl]amino]-2-methylpropionitrile                                     diallate S--(2,3-dichloroallyl)diisopropylthio-                                         carbamate                                                             dicamba  3,6-dichloro- .sub.--o-anisic acid                                    dichloroprop                                                                            2-(2,4-dichlorophenoxy)propionic acid                                 diclofop 2-[4-(2,4-dichlorophenoxy)phenoxy]-                                            propanoic acid                                                        difenzoquat                                                                             1,2-dimethyl-3,5-diphenyl-1H--pyrazolium                              dinoseb  2-sec-butyl-4,6-dinitrophenol                                         diuron   3-(3,4-dichlorophenyl)-1,1-dimethylurea                               DOWCO    2-(4-(3-chloro-5-fluoromethylpyridin-                                 453 ME   2-yloxy)phenoxy)propanoic acid, methyl                                         ester                                                                 EPTC     S--ethyl-dipropylthiocarbamate                                        fenoxaprop                                                                              ethyl 2-(4-(6-chloro-2-benzoxazolyloxy)-                              ethyl    phenoxy)propanoate                                                    flamprop N--benzoyl-N--(3-chloro-4-fluorophenyl)-DL-                                    alanine                                                               fluazifop-                                                                              butyl 2-[4-[5-(trifluoromethyl)-2-                                    butyl    pyridinyloxy]phenoxy]propanoate                                       fluchloralin                                                                            N--(2-chloroethyl)-2,6-dinitro-N--propyl-4-                                    trifluoromethyl)aniline                                               fluometuron                                                                             1,1-dimethyl-3-(α, α, α-trifluoro- .sub.--m-tol              yl)-                                                                           urea                                                                  FMC 57020                                                                               2-(2'-chlorophenyl)methyl-4,4-dimethyl-                                        3-isoxazolidinone                                                     fomesafen                                                                               5-(2-chloro-4-trifluoromethylphenoxy)-                                         N--methylsulfonyl-2-nitrobenzamide                                    fosamine ethyl hydrogen (aminocarbonyl)phosphonate                             glyphosate                                                                              N--(phosphonomethyl)glycine                                           hexazinone                                                                              3-cyclohexyl-6-(dimethylamino)-1-methyl-                                       1,3,5-triazine-2,4(1H,3H)--dione                                      ioxynil  4-hydroxy-3,5-diiodobenzonitrile                                      isoproturon                                                                             N--(4-isopropylphenyl)-N',N'--dimethylurea                            lenacil  3-cyclohexyl-6,7-dihydro-1H--cyclopenta-                                       pyrimidine-2,4(3H,5H)--dione                                          MCPA     [(4-4-chloro- .sub.--o-tolyl)oxy]acetic acid                          MCPB     4-[(4-chloro- .sub.--o-tolyl)oxy]propionic acid                       mefluidide                                                                              N--[2,4-dimethyl-5-[[(trifluoromethyl)-                                        sulfonyl]amino]phenyl]acetamide                                       methabenz-                                                                              1,3-dimethyl-3-(2-benzothiazolyl)urea                                 thiazuron                                                                      methoxuron                                                                              N'--(3-chloro-4-methoxyphenyl)N,N--                                            dimethylurea                                                          metolachlor                                                                             2-chloro-N--(2-ethyl-6-methylphenyl)-N--(2-                                    methoxy-1-methylethyl)acetamide                                       MSMA     monosodium methanearsonate                                            neburon  1-butyl-3-(3,4-dichlorophenyl)-1-methyl-                                       urea                                                                  oryzalin 3,4-dinitro-N,N--dipropylsulfanilamide                                paraquat 1,1'-dimethyl-4,4'-bipyridinium ion                                   pendimethalin                                                                           N--(1-ethylpropyl)-3,4-dimethyl-2,6-di-                                        nitrobenzeneamine                                                     profluralin                                                                             N--(cyclopropylmethyl)-α,α,α-trifluoro-                      2,6-dinitro-N--propyl- .sub.--p-toluidine                             propanil 3',4'-dichloropropionalide                                            sethoxydim                                                                              2-[1-(ethoxyimino)butyl]-5-[2-(ethyl-                                          thio)propyl]-3-hydroxy-2-cyclohexene-                                          1-one                                                                 siduron  1-(2-methylcyclohexyl)-3-phenylurea                                   supriox  2-[1-(2,5-dimethylphenyl)ethylsulfonyl]-                                       pyridine-N--oxide                                                     terbacil 3-tert-butyl-5-chloro-6-methyluracil                                  triallate                                                                               S--(2,3,3-trichloroallyl)diisopropylthio-                                      carbamate                                                             trifluralin                                                                             α,α,α-trifluoro-2,6 dinitro-N,N--dipropyl-                    .sub.--p-toluidine                                                   2,4-D    (2,4-dichlorophenoxy)acetic acid                                      2,4-DB   4-(2,4-dichlorophenoxy)butyric acid                                            3,4-diaryl-4-cyanobutyrates                                                    4-(6-chloroquinoxalinyl-2-oxy)phenoxy-                                         propionate C.sub.1 -C.sub.5 alkyl esters, such                                 as methyl ester, butyl ester, ethyl                                            ester, pentyl ester                                                            ethoxyethoxyethyl 4-(6-chloroquinoxalin-                                       yl-2-oxy)phenoxypropionate                                                     propargyl 2-[4-(3,5-dichloropyridin-2-                                         yloxy)phenoxy]propanoate                                                       methyl 2-[4-(3-chloro-5-trifluoromethyl-                                       pyridin-2-yloxy)phenoxy]propanoate                                    oxyfluorfen                                                                             2-chloro-1-(3-ethoxy-4-nitrophenoxy)-4-                                        (trifluoromethyl)benzene                                              norflurazon                                                                             4-chloro-5-(methylamino)-2-[(3-(tri-                                           fluoro)phenyl]-3(2H)--pyridazinone                                    vernolate                                                                               S--propyl dipropylthiocarbamate                                                ethyl 5-[2-chloro-4-(trifluoromethyl)-                                         phenoxy]-2-nitrobenzoic acid                                          ______________________________________                                    

The compounds of this invention may particularly be useful in combination with the following herbicides for use as pre-emergent treatments for control of weeds in soybeans:

    ______________________________________                                         Common Name  Tradename  Chemical Name                                          ______________________________________                                         chloramben   Amiben ®                                                                              3-amino-2,5-dichloro-                                                          benzoic acid                                           linuron      Lorox ®                                                                               3-(3,4-dichlorophenyl)-1-                                                      methoxy-1-methylurea                                   metribuzin   Lexone ®                                                                              4-amino-6-tert-butyl-3-                                                        (methylthio)-as-tri-                                                           azin-5(4H)one                                          AC 252,214   --         2-(4,5-dihydro-4-methyl-                                                       4-(1-methylethyl)-5-                                                           oxo-1H--imidazol-2-yl)-                                                        3-quinolinecarboxylic                                                          acid                                                   fomesafen    Flex ® 5-(2-chloro-4-trifluoro-                                                       methylphenoxy)-N--                                                             methylsulfonyl-2-nitro-                                                        benzamide                                              lactofen     --         1'-(carboethoxy)ethyl-5-                                                       (2-chloro-4-(trifluoro-                                                        methyl)phenoxy)-2-                                                             nitrobenzoate                                          ______________________________________                                    

Also preferred are mixtures of some of the compounds of this invention with other sulfonylurea herbicides which may be useful for controlling weeds in soybeans. An example of such a sulfonylurea herbicide is:

2-hydroxy-N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]benzenesulfonamide, 1-propanesulfonate.

The herbicidal properties of the subject compounds were discovered in a number of greenhouse tests. The test procedures and results are shown below.

Test A

Seeds of crabgrass (Digitaria sp.), barnyardgrass (Echinochloa crusgalli), wild oats (Avena fatua), sicklepod (Cassia obtusifolia), morningglory (Ipomoea sp.), cocklebur (Xanthium sp.), sorghum, corn, soybean, rice, wheat and nutsedge tubers (Cyperus rotundus) were planted in a growth medium and treated pre-emergence with the chemicals dissolved in a non-phytotoxic solvent. At the same time, cotton having five leaves (including cotyledonary ones), bush beans with the third trifoliolate leaf expanding, crabgrass, barnyardgrass and wild oats with two leaves, cassia with three leaves (including cotyledonary ones), morningglory and cocklebur with four leaves (including the cotyledonary ones), sorghum and corn with four leaves, soybean with two cotyledonary leaves, rice with three leaves, wheat with one leaf, and nutsedge with three to five leaves were sprayed. Treated plants and controls were maintained in a greenhouse for sixteen days, whereupon all species were compared to controls and visually rated for response to treatment. The ratings are based on a numerical scale extending from 0=no injury, to 10=complete kill. The accompanying descriptive symbols have the following meanings:

C=chlorosis or necrosis;

D=defoliation;

E=emergence inhibition;

G=growth retardation;

H=formative effects;

S=albinism;

U=unusual pigmentation;

X=axillary stimulation; and

6Y=abscised buds or flowers.

The ratings for the compounds tested by this procedure are presented in Table A.

                  TABLE A                                                          ______________________________________                                         Structures                                                                                             m.p. (°C.)                                      ______________________________________                                         Compound 1                                                                      ##STR127##                                                                    Compound 2                                                                      ##STR128##                                                                    Compound 3                                                                      ##STR129##                                                                    Compound 4                                                                      ##STR130##                                                                    Compound 5                                                                      ##STR131##                                                                    Compound 6                                                                      ##STR132##                                                                    Compound 7                                                                      ##STR133##                                                                    Compound 8                                                                      ##STR134##                                                                    Compound 9                                                                      ##STR135##                                                                    Compound 10                                                                     ##STR136##                                                                    Compound 11                                                                     ##STR137##                                                                    Compound 12                                                                     ##STR138##                                                                    Compound 13                                                                     ##STR139##                                                                    Compound 14                                                                     ##STR140##                                                                    Compound 15                                                                     ##STR141##                                                                    Compound 16                                                                     ##STR142##                                                                    Compound 17                                                                     ##STR143##                                                                    Compound 18                                                                     ##STR144##                                                                    Compound 19                                                                     ##STR145##                                                                    Compound 20                                                                     ##STR146##                                                                    Compound 21                                                                     ##STR147##                                                                    Compound 22                                                                     ##STR148##                                                                    Compound 23                                                                     ##STR149##                                                                    Compound 24                                                                     ##STR150##                                                                    Compound 25                                                                     ##STR151##                                                                    Compound 26                                                                     ##STR152##                                                                    Compound 27                                                                     ##STR153##                                                                    Compound 28                                                                     ##STR154##                                                                    Compound 29                                                                     ##STR155##                                                                    Compound 30                                                                     ##STR156##                                                                    Compound 31                                                                     ##STR157##                                                                    Compound 32                                                                     ##STR158##                                                                    Compound 33                                                                     ##STR159##                                                                    Compound 34                                                                     ##STR160##                                                                    Compound 35                                                                     ##STR161##                                                                    Compound 36                                                                     ##STR162##                                                                    Compound 37                                                                     ##STR163##                                                                    Compound 38                                                                     ##STR164##                                                                    Compound 39                                                                     ##STR165##                                                                    Compound 40                                                                     ##STR166##                                                                    Compound 41                                                                     ##STR167##                                                                    Compound 42                                                                     ##STR168##                                                                    Compound 43                                                                     ##STR169##                                                                    Compound 44                                                                     ##STR170##                                                                    Compound 45                                                                     ##STR171##                                                                    Compound 46                                                                     ##STR172##                                                                    Compound 47                                                                     ##STR173##                                                                    Compound 48                                                                     ##STR174##                                                                    Compound 49               85                                                    ##STR175##                                                                    Compound 50               .sup.  182-189(d)                                     ##STR176##                                                                    Compound 51               186-190                                               ##STR177##                                                                    Compound 52               150-153                                               ##STR178##                                                                    Compound 53               130(d)                                                ##STR179##                                                                    Compound 54               149-152                                               ##STR180##                                                                    Compound 55               146-149                                               ##STR181##                                                                    Compound 56               146-149                                               ##STR182##                                                                    Compound 57               136-146                                               ##STR183##                                                                    Compound 58               152-156                                               ##STR184##                                                                    Compound 59               185-188                                               ##STR185##                                                                    Compound 60               83-85                                                 ##STR186##                                                                    Compound 61                95-100                                               ##STR187##                                                                    Compound 62               181-183                                               ##STR188##                                                                    Compound 63               135-138                                               ##STR189##                                                                    Compound 64               135-138                                               ##STR190##                                                                    Compound 65               158-163                                               ##STR191##                                                                    Compound 66               156-158                                               ##STR192##                                                                    Compound 67               118-119                                               ##STR193##                                                                    Compound 68               141-143                                               ##STR194##                                                                    Compound 69               144-146                                               ##STR195##                                                                    Compound 70               85-90                                                 ##STR196##                                                                    Compound 71               90-95                                                 ##STR197##                                                                    Compound 72               120-128                                               ##STR198##                                                                    Compound 73               133-138                                               ##STR199##                                                                    Compound 74               133-138                                               ##STR200##                                                                    Compound 75               127-133                                               ##STR201##                                                                    Compound 76               148-154                                               ##STR202##                                                                    Compound 77               179-185                                               ##STR203##                                                                    Compound 78                                                                     ##STR204##                                                                    Compound 79                                                                     ##STR205##                                                                    ______________________________________                                    

    TABLE A        Cmpd. 1 Cmpd. 2 Cmpd. 3 Cmpd. 4 Cmpd. 5 Cmpd. 6 Cmpd. 7 Cmpd. 8 Cmpd.      9 Cmpd. 10 Cmpd. 11 Cmpd. 12 Cmpd. 13 Cmpd. 14 Rate kg/ha .05 .05 .05      .05 .05 .05 0.4 0.4 0.4 0.4 0.4 0.4 0.4 .05        POST-EMERGENCE Bush bean 4C,9G,6Y 5C,9G,6Y 9C 3C,9G,6Y 9C 9C 9C 9C 9C      9C 9C  9C 9C 9C Cotton 2C,2H,5G 2C,3H,6G 6C,9G 4C,9H 4C,9G 3C,2H,9G 9C      6C,9G 4C,9H 3C,8G 4C,9G 9C 5C,9G 6C,9G Morningglory 1C,3G 1C,5G 2C,5G      3C,7H 2C,8G 2C,8H 9C 4C,9G 3C,7G 2C,8G 3C,8H 5C,9G 2C,8H 2C,8G Cocklebur      2C,9G 2C,8G 9C 3C,9H 5C,9G 5C,9G 10C 10C 5C,9G 10C 10C 10C 6C,9G 10C      Sicklepod 1C 2C,5G 5C,9G 3C,6G 2C,5G 3C,7G 9C 3C,5G 4C,7G 3C,5H 2C,5G      2C,6G 5C,9G 5C,9G Nutsedge 0 1C,3G 3C,9G 2C,8G 10C 10C 10C 10C 2C,8G 9C      3C,9G 9C 9C 5C,9G Crabgrass 1C,5G 5G 4C,9G 2C,6G 6C,9G 1C,2H 9C 10C      2C,7G 1C,8G 2C,8G 9C 3C,8G 4C,9G Barnyardgrass 2C,9H 2C,9H 9C 5C,9H 9C      3C,9H 9C 10C 9C 9C 6C,9H 9C 10C 9C Wild Oats 1C,3G 2C,8H 9C 3C,8H 2C,9G      3C,9G 9C 5C,9G 2C,9G 3C,9G 3C,9G 9C 9C 9C Wheat 7G,5X 2C,8H 3U,9G 2C,8H      3C,9G 2C,8G 5U,9G 2C,8G 2C,9G 2C,9G 3C,9G 2C,8G 9C 4C,9G Corn 2U,9H      5U,9C 9C 5U,9C 5U,9G 3U,9G 10C 10C 6U,9C 7U,9C 7U,9G 10C 10C 10C Soybean      1G 2C,7G 6C,9G 5C,8H,5X 5C,9G 2C,9G 9C 9C 6U,9G 9C 5C,9G 9C 9C 9C Rice      7G 6C,9G 6C,9G 5C,9G 5C,9G 4C,9G 6C,9G 6C,9G 6C,9G 5C,9G 9C 9C 9C 6C,9G      Sorghum 9G 4U,9C 5U,9C 3U,9G 6U,9G 3U,9G 9C 9C 6U,9G 10C 10C 10C 9C 10C      Sugar beet PRE-EMERGENCE Morningglory 6G 3C,5G 8H 3C,5H 8G 1C 2C,9H      4C,9H 8G 8G 7G 9H 8H 8G Cocklebur 9H 9H 9H 1H 9H 9H -- 9H 9H 5C,9H 9H 9H      9H 9H Sicklepod 0 7G 2C,7G 1C 8G 2C,5G 5C,9G 2C,8G 5G 2C,8G 2C,7G 2C,8G      1C,3G 4C,9G Nutsedge 0 2C,8G 10E 2C,8G 10E 1C,7G 10E 10E 3C,9G 2C,7G      2C,8G 10E 2C,9G 10E Crabgrass 1C,4G 2C 3C,9G 1C 2C,5G 1C 3C,9H 3C,9G      1C,4G 2C,5G 2C,5G 2C,8G 3C,6G 3C,8G Barnyardgrass 4C,7H 3C,9H 6C,9H      3C,9H 5C,8H 2C,6H 5C,9H 3C,9H 5C,9H 5C,9H 3C,9H 2C,9H 5C,9G 5C,9H Wild      Oats 2C,7G 2C,9G 5C,9H 2C,9G 2C,9G 2C,8G 4C,9H 3C,9H 2C,9G 2C,9H 9G      3C,9G 3C,9H 4C,9H Wheat 2C,8G 2C,9G 9H 9G 1C,8G 1C,7G 9H 9H 9H 2C,9G 9G      2C,8G 3C,9G 2C,9H Corn 2C,6G 2C,9G 10E 2U,9G 2C,9H 2C,8H 10H 10E 5C,9G      3C,9H 6C,9G 10H 2C,9G 10E Soybean 0 1H 2C,7G 6G 2C,3H 1H 9H 9H 3C,8H      3C,4H 3C,7H 9H 6H 2C,8H Rice 8H 9H 10E 2C,8H 10E 3C,6G 10E 10E 10E 5C,9H      9H 10E 5C,9H 9H Sorghum 2C,8H 5C,9G 10H 2C,9G 2C,9H 2C,9H 7C,9H 3C,9H      10H 10H 4C,9H 5C,9H 2C,9G 3C,9H Sugar beet Cotton         Cmpd. 15 Cmpd. 16 Cmpd. 17 Cmpd. 18 Cmpd. 19 Cmpd. 20 Cmpd. 21 Cmpd.      22 Cmpd. 23 Cmpd. 24 Cmpd. 25 Cmpd. 26 Cmpd. 27 Rate kg/ha .05 0.05 0.05      0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05        POST-EMERGENCE Bush bean 9C 4C,9G,6Y  9C 4S,7G,6Y 4S,2H,6Y 5C,9G,6Y      5C,9G,6Y 9C 4C,9G,6Y 6C,9G,6Y 5C,6G,6Y 5C,9G,6Y  4C,9G,6Y Cotton 8C      2C,3H,8G 5C,9G 2C,4G 3C 3C,5G 2C,4G 1C,3G 1C,6G 4C,7G 2C,3G 4C,5G 2C      Morningglory 3C,7G 3C,9G 5C,9G 3C,6G 3C,8H 3C,9G 3C,8H 2C,8G 5C,8H 4C,9G      4C,8H 5C,8G 2C,2H Cocklebur 10C 1C,9G 9C 4C,8G 2C,2G 1C,9G 4C,9G 8H      5C,9G 4C,9G 2C,5G 5C,9G 3C,8H Sicklepod 5C,9G 3C,8G 6C,9G 2C,3H 2C 3C,5G      5C,9G 3C,9G 4C,9H 3C 2C 3C 2C Nutsedge 10C 5G 5C,9G 5G 0 2C,9G 2C,9G 9G      9G 0 0 9G 0 Crabgrass 9C 7G 5C,9G 2G 1C 6G 3C,8G 9G 5C,9G 3C,7G 0 2C,8G      0 Barnyardgrass 9C 2C,9H 9C 2C,8H 2C,6H 5C,9H 5C,9H 3C,9H 5C,9H 9C 2C,9H      9C 2C,4H Wild Oats 4C,9G 2C,9G 5C,9G 2G 4G 2C,9G 3C,9G 3C,9G 4C,9H 7G 3G      9G 0 Wheat 5C,9G 3C,9G 4C,9G 2G 3G 2C,9G 9G 2C,9G 4C,9G 5G,5X 3G,5X      2C,9G 0 Corn 10C 9C 9C 2C 2C,7H 2C,8H 7U,9C 9C 9C 7U,9C 2C,7H 5U,9C 0      Soybean 9C 2C,9G 5C,9G 2C,4G 1C 2C,9G 2C,8G,5X 9C 3C,8H 5C,9G 1C,1H      4C,8G 4G Rice 4C,9G 5C,9G 6C,9G 2C,6G 2C,8G 5C,9G 5C,9G 5C,9G 5C,9G      6C,9G 2C,8G 6C,9G 4G Sorghum 10C 4C,9G 9C 2C,6H 1C,9G 2C,9H 3C,9G 3C,9G      3C,9G 4C,9G 9G 3U,9G 2C,7H Sugar beet  4C,9G 9C 2C,2H 1C,5H 2C,7G 5C,9H      4C,9G 4C,9G 3C,7H 1C,4H 9C 0 PRE-EMERGENCE Morningglory 8G 9G 9C 2C,5H      1C,2H 9G 8H,2C 9G 9G 9G 2C,5H 9C 2C,4G Cocklebur 9H 7H 9H -- 0 9H 9H 9H      9H 9H 7H 8H 8H Sicklepod 3C,8G 7H 9G 2C 0 5G 1C 6G 5G 8G 2C 8H 1C      Nutsedge 10E 4G 10E 0 0 2C,6G 10E 10E 10E 5G 0 10E 0 Crabgrass 3C,8H 2G      5G 0 0 1C 1C,4G 2C,8G 2C,5G 2G 0 2C,6G 1C Barnyardgrass 5C,9H 8H 9H 2C      1C 5C,9H 5C,9H 2C,5G 4C,9H 2C,8G 2C,5G 4C,9H 3C,5G Wild Oats 5C,9H 8G      2C,9G 1C,4G 4G 2C,8G 2C,7G 3C,8G 4C,8H 8G 1C,5G 4C,9H 2C,5G Wheat 9H 9G      5C,9H 3G 4G 2C,8G 9H 9H 4C,9H 7G 1C,5G 9H 5G Corn 10H 9H 10H 2C 2C,9H      1C,7G 3C,9G 5C,9H 9H 9G 2C,8H 4C,9H 2C,4G Soybean 9H 1C,1H 9H 2G 0 0 0      3C,5H 2C,2H 3C,8H 2G 5G 0 Rice 10E 9H 10E 2G 5G 4C,9H 5G 10E 9H 10E      1C,4G 10E 3C Sorghum 5C,9H 9H 10H 1C,3G 2C,9H 2C,8G 3C,9H 7C,9H 5C,9H      3C,9H 4C,9H 10H 2C,5G Sugar beet  8G 5C,9G 1C,3H 0 8G 0 10E 10E 5G 0      5C,9G 3C,6G Cotton         Cmpd. 28 Cmpd. 29 Cmpd. 30 Cmpd. 31 Cmpd. 32 Cmpd. 33 Cmpd. 34 Cmpd.      35 Cmpd. 36 Cmpd. 37 Cmpd. 38 Cmpd. 39 Cmpd. 40 Cmpd. 41 Rate kg/ha 0.05      0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05        POST-EMERGENCE Bush bean 1C 0 9C 9C 9C 9C 5C,9G,6Y 9C 3C,9G,6Y      4S,8G,6Y 5C,9G,6Y 5C,9G,6Y  5S,8G,6Y 3C,9G,6Y Cotton 0 0 5C,9G 3C,5G      5C,9G 3C,9G 4C,9G 4C,9G 3C,3H,9G 3C,8G 4C,9G 3C,3H,6G 2C 3C,2H Morningglo      ry 0 0 9C 3C,5G 5C,9G 2C,8G 3C,5G 9C 3C,7H 3C,7H 5C,9G 3C,8H 2C,5G 2C,5G      Cocklebur 3H 0 10C 9H 10C 9G 3C,9G 2C,9G 2C,2H 2C,3G 5C,9G 3C,6G 2C      3C,5H Sicklepod 0 0 4C,7G 1C,3G 9C 4C 2C 2C,7G 2C 2C 4C,8G 2C,5G 3C,5G      2G Nutsedge 0 0 5C,9G 3C,7G 2C,9G 5G 2C,9G 9G 0 0 3G 0 4G 3G Crabgrass 0      0 3C,9G 2C,5G 6C,9G 6G 1C,5G 9G 1C,3G 0 2C,5G 1C 3C,5G 1C,5G Barnyardgras      s 2H 0 9C 9C 9C 6C,9H 5C,9H 9C 1C,3G 1C 9C 5C,9H 4C,9H 9H Wild Oats 0 0      5C,9G 3C,9G 9C 2C,9G 1C,8G 3C,9G 5G 2G 1C 0 0 2G Wheat 0 0 4C,9G 2C,9G      9C 9G 4C,9H 3G 0 0 3G 0 0 4G Corn 0 0 10C 9C 9C 5C,9G 3C,9H 9C 3C,9H      2C,8H 8U,9C 8U,10C 3U,9C 2C,8H Soybean 0 0 4C,9H 2C,8H 5C,9G 4C,9G      3C,9G,7X 5C,9G 3C,7G,5X 1C,3G 4C,9G 2C,5H 2C,5H 0 Rice 0 0 5C,9G 5C,9G      9C 5C,9G 6C,9G 5C,9G 2C,7G 2C,9G 3C,8G 2C,6G 2C,8G 2C,9G Sorghum 6G 0      10C 10C 9C 3C,9G 4C,9G 2C,9G 2C,9G 2C,9H 2C,9G 2C,9G 2C,9G 9G Sugar beet      -- -- -- -- -- -- 2C,7G -- -- -- -- -- -- -- PRE-EMERGENCE Morningglory      0 0 3C,9H 5G 9G 8G 1C,4H 9G 0 0  8G 7G 9G 1H Cocklebur 8H 0 9H -- 9H --      9H 9H 0 0 7H 0 0 8H Sicklepod 2H 5H 3C,8G 2C,7G 9G 8G 0 7G 1C 0 5G 0 0 0      Nutsedge 0 0 2C,9G 2C 10E 10E 2C,8G 10E 0 0 0 0 0 0 Crabgrass 2G 0 3C,8H      2C,5G 3C,9G 4C,6G 1C,3G 3C,9G 4G,2C 1C 1C,3G 0 1C 1C Barnyardgrass 2G 0      5C,9H 5C,9H 3C,9H 5C,9H 3C,9H 2C,9H 2C 1C 9G,4C 2C,8G 2C,7G 3C Wild Oats      0 0 5C,9G 5C,9H 3C,9H 2C,8G 2C,8H 2C,7G 1C,3G 1C 1C,5G 4G 1C 1C Wheat 0      0 9H 9H 5C,9H 2C,8H 3C,9H 1C,5G 0 0 4G 2G 3G 6G Corn 2G 0 9G 9H 9H 2C,9G      3C,9H 2C,9G 2C,9G 2C,9H 2C,9G 4C,9G 2C,9G 2C,4G Soybean 0 0 3C,8H 3C,6G      9H 9H 1C,1H 9H 1C 2G 1C,2G 1C 1H 0 Rice 5G 0 10E 5C,9G 10E 10E 3C,8H 10E      1C,3G 2G 4C,7H 3C,7H 3C,6G 3C,8H Sorghum 2G 0 5C,9H 5C,9H 3C,9H 5C,9H      3C,9H 9G 2C,9H 2C 5C,9G 3C,9G 5C,9H 3C,9H Sugar beet -- -- -- -- -- --      8H -- -- -- -- --  -- -- Cotton         Cmpd. 42 Cmpd. 43 Cmpd. 44 Cmpd. 45 Cmpd. 46 Cmpd. 47 Cmpd. 48 Cmpd.      49 Cmpd. 50 Cmpd. 51 Cmpd. 52 Cmpd. 53 Cmpd. 54 Rate kg/ha 0.05 0.05      0.05 0.05 0.05 0.05 0.05 50 50 50 50 50 50        POST-EMERGENCE Bush bean 10D,9G,6Y 9D,9G,6Y 5C,9G,6Y 3C,9G,6Y 9C      5C,9G,6Y 5C,9G,6Y 5C,9G,6Y 4C,9G,6Y 4C,7G,6Y 9C 5C,9G,6Y -- Cotton 4C,8G      5C,9G 3C,7G 2C,4G -- -- -- 4C,9G 4C,5H,9G 3C,8G 9C 5C,9G 4C,9G Morningglo      ry 9C 3C,8H 1H 1C 10C 10C 5C,9H 5C,9G 4C,9G 3C,8G 5C,9G 5C,9G 6C,9G      Cocklebur 9C 6C,9G 5C,9G 4C,9G 10C 10C 5C,9H 4C,9G 9C 7G 2C,9G 9C 5C,9G      Sicklepod 3C 3C,6H 5G 3C,4H 9C 4C,8H 3C 3C,9G 3C,7G 1C,3G 3C,3H 2C,5G      3C,7H Nutsedge 1C,9G 9G 0 2C,8G 2C 3C,8G 3C,9G 2C,9G 6C,9G 3G 3C,8G      2C,9G 3G Crabgrass 2C,6G 2C,8G 2C,6G 3G 9C 4C,9G 4C,9G 3C,9G 2C,8G 2C,7G      2C,8G 3C,9G 3C,5G Barnyardgrass 3C,9H 4C,9H 2C,8H 1H 9C 5C,9G 5C,9H      3C,9H 9C 3C,9H 9C 5C,9H 5C,9H Wild Oats 9G 2C,9G 2C,5G 4G 9C 4C,9H 2C,9H      2C,9G 3C,9G 9G 3C,9G 2C,9H 4C,9G Wheat 1C,9G 3C 1C,5G 5G 6C 2C,7G 4C,9G      9C 3C,9G 9G 2C,9G 2C,9G 4C,9G Corn 3C,8H 3C,9H 1U,9G 1C,9G 5C 9G 2C,9H      3C,9H 4C,9G 5C,9G 9C 5C,9G 5U,9G Soybean 5C,9G 9C 4G 2C,9G 10C 3C,8H      5C,9G 4C,9G 3C,9G 3C,9G 3C,9G 5C,9G 4C,9G Rice 5C,9G 6C,9G 3C,9G 2C,8G      6C 6C,9G 5C,9G 6C,9G 4C,9G 5C,9G 4C,9G 6C,9G 5C,9G Sorghum 9G 2C,9G 9G      2C,9H 6C 4C,9G 3C,9G 9C 4C,9G 5C,9G 9C 4C,9G 5C,9G Sugar beet -- -- --      -- -- -- -- 9C 2C,8G 3C,8H 9C 4C,8H 5C,9G PRE-EMERGENCE Morningglory 8G      9G 5G 0 10C 8H 8H 9G 8G 9C 8G 4C,8H 2C,9G Cocklebur 8H 8H 9H 8H 9H 9H 9H      9H 2G -- 2C,6H -- 9H Sicklepod 9C 9G 7G 6G 4C,9G 5H 2C 9G 2C,3G 3C,5G 2C      2C 9G Nutsedge 7G 9G 5G 0 10E 10E 10E 10E 9G 2C,5G 2C,6G 5C,9G 4G      Crabgrass 5C,8G 4C,8G 2C,8G 1C 5C,9G 3C,5G 4C,7G 2C,7G 2C,5G 2C,4G 2C,5G      2C,5G 3C,8G Barnyardgrass 3C,8G 5C,9H 2C,9H 2C 5C,9H 4C,9H 5C,9H 5C,9H      3C,8H 3C,9G 4C,9G 4C,8G 3C,9H Wild Oats 6G 2C,6G 0 2C 4C,8H 3C,8H 3C,8G      3C,9H 3C,9G 2C,8G 3C,8G 2C,9G 3C,9G Wheat 8G 2C,9H 8G 5G 3C,9H 9H 2C,9H      3C,9H 2C,9G 2C,9H 3C,9G 2C,9G 5C,9H Corn 2C,7G 8G 3C,7G 2C,8G 3C,9H      4C,9H 3C,9G 3C,9H 2C,9G 5C,9H 3C,9H 3C,9G 4C,9G Soybean 6H 6H 0 2H 8H 1H      2H 3C,8G,7X 2C,2H 3C,6G 2C,8G 3C,5H 3C,4H Rice 8H 9H 9H 5G 10E 4C,7H      3C,6H 10E 10E 3C,9H 5C,9H 3C,8H 4C,9G Sorghum 2C,9G 5C,9H 2C,9H 2C,6G      10H 5C,9H 3C,9H 3C,9H 6C,9H 6C,9H 4C,9H 5C,9G 5C,9G Sugar beet -- -- --      -- -- -- -- 5C,9G 9C 3C,9G 5C,9G 4C,8G 9C Cotton        -- -- -- -- --      9G  Cmpd. 55 Cmpd. 56 Cmpd. 57 Cmpd. 58 Cmpd. 59 Cmpd. 60 Compound 61      Cmpd. 62 Cmpd. 63 Cmpd. 64 Cmpd. 65  Cmpd. 66 Cmpd. 67 Cmpd. 68 Rate      kg/ha 50 50 50 50 50 50 50 400 50 50 50 50 50 50 50        POST-EMERGENCE Bush bean -- -- -- -- -- 6C,9G,6Y -- -- -- -- --  -- --      -- -- Cotton 9C 6C,9G 3C,8H 4C,8G 4C,8H 4C,5H 1B 1B 2C,9H 9G 5C,9G 3C,8H      3C,8G 2C,9G 3C,9G Morningglory 4C,8H 5C,9G 3C,6H 3C,6H 4C,7H 3C,4G      1C,3G,1B 1B 2H 3C,6G 2C,8G 2C,7H 2C,3G 3C,7H 4G Cocklebur 10C 10C 4C,9H      3C,9H 4C,8H 5C,9G 1B 1B 3C,9H 4C,9H 3C,9H 2C,7H 4C,8G 5C,9G 9C Sicklepod      5C,9G 9C 5C,9G 3C,3H 9C 2C,4G 1B 1B 3C,6H 2C,3G 3C,8H 2C,5G 3C,6H 3C,4G      3C,4G Nutsedge 2C,9G 3C,8G 0 2G 4C,8G 3C,9G 0 0 0 2C,7G 3C,9G 2G 3G      0C,7G 5C,9G Crabgrass 2C,6G 3C,7G 1C,5G 2C,6G 2C,7G 2C,3H 0 1B 0 0 4G 2G      0 3H 4C,6G Barnyardgrass 5C,9G 9C 2C,9H 2C,9H 4C,9H 3C,8H 0 1B 7H 9H      2C,9H 2C,8H 3C,8H 5C,9H 9G Wild Oats 3C,9G 5C,9G 3C,4G 2C 4C,9G 2C,6G 0      1B 1C 6G 0 0 3G 3C,9G 4C,9G Wheat 9C 5C,9G 5G 1C,2G 5C,9G 2C 0 1B 0 0      2C,7G 0 2G 5G 4C,9G Corn 5C,9G 9C 2C,5G 3C,9G 4C,9G 3C,9G 0 1B 2C,7H      3C,9H 3C,9H 3C,8H 3C,8H 5C,9G 10C Soybean 5C,9G 5C,9G 3C,9G 3C,7G 4C,9G      2C,8G 2G,1B 1B 4C,9G 4C,9G 3C,9G 4C,9G 3C,8G 3C,8H 4C,9G Rice 6C,9G      5C,9G 5C,9G 5C,9G 4C,9G 2C,6G 0 1B 7G 7G 5C,9G 2C,8G 9G 2C,8G 9C Sorghum      6C,9G 4C,9G 2C,9H 2C,7H 3C,8G 3C,9G 0 1B 3C,9H 3C,9H 3C,9G 3C,9H 3C,9H      4C,9G 10C Sugar beet 5C,9G 9C 3C,8G 5C,9G 4C,8G 1H 0 1B 1C,3G 3C,6H      3C,5G 2C,3G 2C,6G 4C,6G 9C PRE-EMERGENCE Morningglory 6G 9G 3C,9H 9H 9H      0 0 0 2C,3H 2C,5H 2C,7G 7H  0 3C,3H 3G Cocklebur 9H 9H 9H 9H 9H 2C,6H 0      0 2C 2C,4H 2C,8H 2H 3C,5H 2C,5H 5C,9H Sicklepod 9G 9G 2C 9G 4C,8H 0 0 0      0 0 3C,6G 0 2C 2G 4C,7G Nutsedge 9G 8G 5G 2C,7G 0 2C,6G 0 0 0 8G 8G 5G 0      0 10E Crabgrass 5G 2C,7G 2C,4G 2C,5G 2C,6G 1C 0 0 0 0 2G 2G 0 0 3G      Barnyardgrass 5C,9H 3C,9H 3C,7H 4C,8G 2C,7G 2C,6H 0 0 0 2C,7G 3C,8H 3H 0      3C,8H 9H Wild Oats 3C,9G 2C,9G 3C,8G 2C,8G 3C,8H 2C,8G 0 0 0 3C,8H 3C,8G      2C,4G 0 3C,8G 3C,9G Wheat 2C,9G 5C,9H 7G 6G 8G 8G 0 0 0 5G 3C,8H 2G 0 8G      2C,9G Corn 2C,9G 3C,9G 2C,7G 2C,9G 3C,8G 5C,9H 0 0 2C,8H 3C,9H 3C,9G      2C,8H 3C,9H 9G 5C,9H Soybean 2C,7H 3C,6H 2C,2H 2C,8G 3C,5G 0 0 0 0 0      2C,6H 1C 0 3C,3H 2C,8G Rice 4C,9H 5C,9G 3C,8H 3C,9H 3C,9H 2C,6G 0 0 2G      3C,5G 3C,8H 2C,3G 2C,3G 4C,5G 3C,5G Sorghum 4C,9H 5C,9G 2C,9H 2C,8H      3C,9H 5C,9H 0 0 2C,7H 9H 4C,9H 3C,8H 3C,8G 4C,9G 6C,9H Sugar beet 4C,9G      9C 4C,8G 10E 3C,8G 2G 0 0 3H 6G 9G 8G 0 2C,4G 5C,9G Cotton 9G 9G 2C,6G      9G 3C,5G -- -- -- 0 5G 8G 6G 0 6H 8G         Cmpd. 69 Cmpd. 70 Cmpd. 71 Cmpd. 72 Cmpd. 73 Cmpd. 74 Cmpd. 75 Cmpd.      76 Cmpd. 77 Cmpd. 78 Cmpd. 79 Rate g/ha 50 50 50 50 50 50 50 50 50 50      50   POST-EMERGENCE Bush bean -- -- -- -- -- -- -- -- -- -- -- Cotton      5C,9G 5C,9G 9C 2G 3C,9G 2C,5H 3C,8H 1C 2C,5G 4C,9G 4C,8H Morningglory      5C,9G 2C,5G 3C,7H 1H 2C,5G 4G 4C,9G 1C,4G 2C,3H 4C,8H 4C,8H Cocklebur 9C      10C 10C 4C,8H 9C 5G 3C,9H 2C,8H 1H 3C,8H 5C,9G Sicklepod 3C 2C,4G 5C,8G      4C,6H 9C 3G 3C,8G 1C 2C,3H 4C,5H 4C,8H Nutsedge 4C,9G 10C 10C 3G 6C,9G      2G 2C,5G 0 0 2C,4G 0 Crabgrass 6H 8G 2C,8G 1C,3G 2C,7G 2G 2H 0 2G 3C      4C,9G Barnyardgrass 9C 4C,9H 3C,8H 2H 9C 9H 9C 3C,9H 2C,8H 5C,9H 5C,9H      Wild Oats 6C,9G 3C,9G 6C,9G 0 9C 0 5C,9G 1C 2G 4C,9H 4C,8H Wheat 6C,9G      9G 9G 3G 9C 0 5C,9G 1C 3G 9G,7X 8G Corn 10C 5C,9G 5U,9C 0 9C 2C,8H 2C,9H      2C,9H 0 5C,9G 3C,9G Soybean 4C,9G 3C,9G 3C,9G 3C,8H 4C,9G 3C,6H 3C,9G      3C,7H 2H 4C,9G 4C,9G Rice 9C 5C,9G 5C,9G 2C,7G 5C,9G 2C,8G 6C,9G 4C,9G      2C,9G 5C,9G 5C,9G Sorghum 3U,9C 3U,9G 10C 3C,7G 9C 3C,9H 10C 3C,9H 0C,8H      3C,9G 3C,9G Sugar beet 9C 9C 9C 3C,8G 5C,9G 2C,5G 4C,9G 4C,9G 2H 5C,9G      5C,9G PRE-EMERGENCE Morningglory 8H 0 9C 1C,2H 8H 2C,5G 9G 9G 0 6H 2C,5H      Cocklebur 9H 9H 9C 9H 9H 3C,8H 9H 9H 0 8H 9H Sicklepod 5C,2C 7G 8G 1C 8G      4G 5G 8G 0 3G 2C Nutsedge 10E 10E 10E 0 7G 0 0 0 0 0 0 Crabgrass 5G      2C,4G 3C,5G 0 0 2G 0 0 0 1C 0 Barnyardgrass 3C,9H 3C,8G 3C,8H 2C 3C,9H      1H 2C,3G 2G 0 3C,5H 2C,7G Wild Oats 3C,9G 3C,8G 4C,9G 3C,7G 4C,9G 0      3C,7G 2C,7G 0 4C,8G 2C,4G Wheat 2C,9G 6G 3C,9G 3G 2C,9G 0 2C,8G 2C,6G 0      2C,8G 6G Corn 4C,9G 3C,9H 10E 2C,6H 2C,9G 2C,8H 3C,9H 9G 0 3C,9G 3C,8G      Soybean 3C,8G 5G 3G 1C,1H 8G 0 3C,7H 5G 0 2C,5G 2C,6G Rice 4C,7G 3C,6H      3C,8H 2C,3H 10E 2C,4G 3C,8H 2C,8G 0 2C,7H 2C,6G Sorghum 6C,9H 6C,9H      5C,9H 3C,8H 3C,9G 2C,4G 2C,9G 2C,5G 0 3C,9G 2C,8H Sugar beet 5C,9G 5C,9G      5C,9G 2C,8G 10E 3G 7G 8G 0 3C,9G 3C,8G Cotton 9G 9G 9G 0 9G 0 4H 7G 0      2C,3G 5G,2C

Test B

Two plastic bulb pans were filled with fertilized and limied Fallsington silt loam soil. One pan was planted with corn, sorghum, Kentucky bluegrass and several grass weeds. The other pan was planted with cotton, soybeans, purple nutsedge (Cyperus rotundus), and several broadleaf weeds. The following grass and broadleaf weeds were planted: crabgrass Digitaria sanguinalis), barnyardgrass (Echinochloa crusgalli), wild oats (Avena fatua), johnsongrass (Sorghum halepense), dallisgrass (Paspalum dilatatum), giant foxtail (Setaria faberii), cheatgrass (Bromus secalinus), mustard (Brassica arvensis), cocklebur (Xanthium pensylvanicum), pigweed (Amaranthus retroflexus), morningglory (Ipomoea hederacea), sicklepod (Cassia obtusifolia), teaweed (Sida spinosa), velvetleaf (Abutilon theophrasti), and jimsonweed (Datura stramonium). A 12.5 cm diameter plastic pot was also filled with prepared soil and planted with rice and wheat. Another 12.5 cm pot was planted with sugar beets. The above four containers were treated pre-emergence with several test compounds within the scope of the invention.

Twenty-eight days after treatment, the plants were evaluated and visually rated for response to the chemical treatments utilizing the rating system described previously for Test A. The data are summarized in Table B. At least one compound exhibits utility for pre-emergence weed control in soybeans and cotton.

    TABLE B       PRE-EMERGENCE ON FALLSINGTON SILT LOAM        Compound 2 Compound 3 Compound 4 Compound 20 Compound 21 Cmpd. 22      Compound 23  Compound 24 Compound 26 Compound 30 Rate kg/ha 0.03 0.12      0.03 0.12 0.03 0.12 0.25 0.063 0.125 0.031 0.125 0.125  0.062 0.031      0.015 0.125 0.031 0.062 0.031 0.125 0.031        Crabgrass 0 0 6G,3C 9G,9C 0 0 9G 6G 2G 0 9G 7G 3G 0 0 0 0 8G 5G 7G,2H      7G Barnyardgrass 3G 6G,3H 8G,3H 10C 0 0 9G,9C 8G 3G 0 5G 7G 2G 2G 0 0 0      9G 5G 9G,9C 9G,5H Sorghum 10C 10C 10E 10E 3G 9G,9C 9G,9C 8G 10C 4G 10C      10C 10C 10C 9G 3C 2C 9G,9C 9G 10E 10E Wild Oats 5G 7G 8G,8C 8G,8C 0 6G      8G 6G 8G 4G 8G 9G 7G 5G 4G 0 0 8G 5G 7G 7G Johnsongrass 8G,7C 9G,9C      9G,8C 10C 0 7G,3H 8G 6G 8G 2G 8G 8G 8G 7G 7G 2C 0 9G,9C 7G 9G,9C 8G,7C      Dallisgrass 4G 6G,3H 8G,3H 10C 0 3G 9G 6G 8G 0 9G 9G,9C 8G 5G 3G 0 0 9G      8G 10C 8G,5H Giant foxtail 0 8G,5H 7G,3H 10C 0 3G 9G 2G 0 2G 2G 9G,9C 5G      0 0 0 0 9G,9C 5G 10C 9G,3H Ky. bluegrass 6G 8G,8C 10C 10C 4G 6G,3C 9C,9G      8G 9G 0 9G 9G,9C 8G 3G 3G 0 0 9G,9C 9G 10C 10C Cheatgrass 9G,9C 9G,9C      8G,8C 10C 0 0 9G 7G 8G 4G 9G 9G 8G 6G 4G 0 0 9G,9C 8G 8G,8C 7G Sugar      beets 0 3G 8G,8C 10C 0 0 8G 6G 3G 2G 8G 6G 5G 5G 4G 2G 0 9G 5G 10C 7G,5H      Corn 3G 8G,5H 4G 10C 0 0 8G,7H 5G 6G,5H 0 9G,9C 8G,7H 6G,5H 2G 2G 0 0 9G      9G 10C 3H,8G Mustard 7G,3H 9G,8C 10C 10C 0 6G,3H 9G 9G 9G 7G 9G,9C 9G 9G      7G 5G 0 0 9G,9C 9G 10C 9G,9C Cocklebur 5G 5G 9G,8C 9G,9C 0 0 -- -- 2G 0      5G 6G 3G 3G 2G 0 0 4G 0 8G,8C 7G,5H Pigweed 0 5G,5C 10C 10C 5G,5C 10C --      -- -- -- -- -- -- -- -- -- -- -- -- -- -- Nutsedge 0 3G 7G 10E 0 0 9G 4G      7G 2G 10C 10C 10C 9G 8G 0 0 10C 9G 10E 9G Cotton 0 2G 5G,3H 7G,5H 0 0 5G      2G 2G 0 6G 6G 2G 2G 2G 0 0 4G 0 8G,5H 6G,3H Morningglory 0 4G 2G 3G 0 2G      8G 5G 0 0 6G 4G 3G 2G 0 0 0 7G 4G 9G,7C 6G,5H Sicklepod 0 4G 3G 3G 0 0      5G 2G 5G 2G 2G 0 0 2G 0 0 0 4G 2G 7G,4C 3G Teaweed 0 0 4G,3H 6G,5H 0 0 0      0 0 0 0 2G 0 0 0 0 0 5G 0 7G,3H 4G Velvetleaf 0 0 3G,5H 7G,5H 0 0 7G 2G      0 0 4G 0 0 0 0 0 0 5G 3G 8G,9C 3G Jimsonweed 0 0 3G 7G 0 0 3G 0 0 0 8G 0      0 0 0 0 0 5G 0 9G,8C 3G Soybean 0 0 3G,3H 6G,5H 0 0 3G,3H 0 0 0 7G,7H 2G      2G 0 0 0 0 4G 2G 6G,5H 2C Rice 7G,4C 10C 9G,9C 10C 4G 6G,3H 10C 8G 7G 4G      10C 10C 9G 6G 6G 2G 0 10E 10E 10E 10E Wheat 5G 7G,3C 8G,5C 10C 0 6G,3C      8G 7G 5G 2G 9G 9G 7G 4G 3G 0 0 5G 3G 9G,9C 7G        Compound 31 Compound 32 Compound 33 Compound 35 Compound 38 Compound      39 Compound 42 Rate kg/ha 0.125 0.031 0.125 0.008 0.031 0.003 0.0015      0.125 0.031 0.125 0.008 0.031 0.003 0.0015 0.25 0.062 0.25 0.062 0.125      0.031        Crabgrass 4G 3G 9G,9C 8G 8G 7G 6G 7G 6G 9G 6G 8G 2G 2G 2G 0 2G 0 2G 2G      Barnyardgrass 9G,5H 7G,3H 9G,9C 6G,3C 7G 3G 2G 5H,7G 3H,6G 8G,8C 3G      5H,7G 2G 2G 6G 3G 5G 0 0 0 Sorghum 10E 10C 10C 10C 10C 10C 10C 10C 10C      10C 8G 10C 4G 2G 8G,8C 8G,5H 8G,5H 2G 10C 2G Wild Oats 7G 7G 7G 6G 6G 6G      5G 6G 2G 6G 0 2G 0 0 0 0 0 0 2G 0 Johnsongrass 8G,3H 6G,3H 9G 6G 8G 6G      6G 7G 5G 10C 0 9G 0 0 5G 4G 0 0 2G 0 Dallisgrass 8G,3H 7G,3H 9G,9C 8G      9G,9C 7G 6G 8G 8G 9G,9C 7G 9G 7G 0 0 0 0 0 0 0 Giant foxtail 9G,9C 8G,5H      10C 6G,2H 9G 6G 6G 5G 4G 10C 2G 8G 2G 0 3G 0 0 0 0 0 Ky. bluegrass 10C      7G,3H 10C -- 10C -- -- 9G,9C 9G,9C 9G,9C 4G 9G,9C 2G 0 -- -- -- -- 4G 0      Cheatgrass 8G,9C 6G 10C 9G,5C 10C 9G 5C,8G 10C 10C 9G,9C 9G 10C 8G 4G 3G      0 0 0 2G 0 Sugar beets 7G,5H 4G 10C 10C 9G,9C 9G 8G,8C 9G,9C 7G 10C 9G      10C 8G 7G 4G 2G 4G 0 3G 0 Corn 9G,9C 5H,7G 9G,9C 9G,9C 9G,9C 7H 5G 8G 5G      8G 7G,5H 6G 3G 2G 8G,8C 5G 7G 0 3G 0 Mustard 9G,9C 10C 9G,9C 9G,7C 9G,9C      9G 9G 8G 6G 9C 9G 9G 9G 8G 0 0 0 0 8G 7G Cocklebur 2G 0 8C 6G,2H 7G --      5G,2H 6G 3G 8G,8C 0 6G 3G 0 0 0 0 0 2G 0 Pigweed -- -- -- -- -- -- -- --      -- -- -- -- -- -- -- -- -- -- -- -- Nutsedge 10E 7G 10C 10C 10C 10C 10C      5G 3G 10C 10C 10C 10C 2G 5G 0 0 0 0 0 Cotton 4G 0 8G,8C 8G 7G 8G 6G,3H      6G,3C 3G 8G,8C 6G 7G 3G 0 0 0 2G 0 2G 2G Morningglory 8G,3H 5G 7G 3G,2C      2G 3C 0 6G 0 8G,8C 7G 4G 3G 0 4G 0 2G 0 0 0 Sicklepod 7G 4G 8G,8C 8G,5C      7G,7C 3G 7G 8G,8C 7G,7C 9G,9C 7G 8G,8C 2G 0 0 0 0 0 0 0 Teaweed 8G,3H 3G      8G 8G,3C 8G 8G 7G 8G 7G 10C 3G 9G 0 0 2G 2G -- 2G -- -- Velvetleaf 4G,3H      3G 10C 8G 9G 7G 6G 7G 10C 10C 5G 10C 2G 0 0 0 7G 0 0 2G Jimsonweed 5G,5C      3G 9G,9C 7G,7H 8G,8C 4G 3G 5G 5G 8G 7G 7G 3G 0 0 0 0 0 0 0 Soybean 2G 0      8G,8C 8G,7H 6G,5C 7G 6G,2C 6G,3C 4G 8G,8C 7G,5H 7G,5C 6G 2G 2G 2G 0 0 2G      2G Rice 10C 8G,5H 10C 10C 10C 10C 10C 10C 10C 10C 10C 10C 10C 9G 6G 3G      5G 0 7G 0 Wheat 7G 5G 8G 8G 3G 7G 6G 6G 2G 5G 4G 0 2G 0 0 0 0 0 0      0        Compound 43 Compound 44 Compound 46 Compound 47 Compound 48      Rate kg/ha 0.125 0.031 0.125 0.031 0.125 0.031 0.015 0.125 0.031 0.015      0.125 0.031 0.015        Crabgrass 3G 2G 5G 2G 9G,7C 8G,7C 7G,7C 5G,3C 2C,2G 0 4G 2G 0 Barnyardg      rass 0 0 0 0 9G,7C 8G,7C 5G,3C 6G,3C 2G,2C 0 6G,5C 4G,3C 2G Sorghum      7G,3H 2G 0 0 10C 10C 10C 9G,9C 7G,5H 3G,3H 9G,9C 9G,9C 8G,8C Wild Oats 0      0 0 0 7G,3C 7G,3C 5G,3C 6G 3G 2G 6G 5G 4G Johnsongrass 0 0 0 0 9G,5C      8G,5C 2G 8G,7C 2G 0 8G 8G 3G,3H Dallisgrass 3G 0 2G 0 9G 9G 8G 8G 5G 0      7G 5G 0 Giant foxtail 0 0 0 0 9G,9C 9G,9C 7G 8G,8C 2G,3C 0 8G,8C 4G,3C 0      Ky. bluegrass 2G 0 0 0 -- -- -- -- -- -- -- -- -- Cheatgrass 4G 2G 0 0      8G 8G 2G 8G 5G 0 8G 6G 0 Sugar beets -- -- -- -- 9G,5C 8G,5C 7G 8G 4G,3H      3G 6G 4G 3G Corn 2G 0 0 0 8G,8C 7G,7H 2G,2C 7G,7H 3G,3C 2G,2H 7G,5C      2G,2C 0 Mustard 7G 5G 5G 0 9G,9C 8G,8C 8G,8C 9G,8C 7G 6G 9G,9C 8G,5C 7G      Cocklebur 2G 0 0 0 6G,3C 2G 2G 6G,7C 0 0 5G,5C 3C,2G 0 Pigweed -- -- --      -- -- -- -- -- -- -- -- -- -- Nutsedge 0 0 0 0 10C 9G 6G -- 0 0 -- 2G 2G      Cotton 5G 2G 3G 0 4G,7H 3G,5H 3G. 7G,3C 3G 3G 3G,3H 2G 2G Morningglory      2G 0 0 0 7G 5G,5H 3G,3H 5G,3H 0 0 5G 3G 0 Sicklepod 0 0 0 0 -- 5G,5H      3G,3H 2G,3C 0 0 2G 0 0 Teaweed -- -- -- -- -- -- -- -- -- -- -- -- --      Velvetleaf 0 0 0 0 -- 2G,2H 2G 5G,3H 0 0 7G,5C 0 0 Jimsonweed 0 0 0 0 --      4G 2G 2G,2C 0 0 2G,2C 0 0 Soybean 0 0 0 0 7H 5G,5H 5G,5H 2G,3C 0 0 2G,3C      0 0 Rice 5G 2G 3G 0 10C 10C 10C 10C 4G 2G 9G 5G 3G Wheat 0 0 0 0 7G 3G 0      7G 4G 2G 5G 4G 4G

Test C

Two ten-inch in diameter plastic pans lined with polyethylene liners were filled with prepared Fallsington silt loam soil. One pan was planted with seeds of wheat (Triticum aestivum), barley (Hordeum vulgare), wild oats (Avena fatua), downy brome (Bromus tectorum), cheatgrass (Bromus secalinus), blackgrass (Alopecurus myosuroides), annula bluegrass (Poa annua), green foxtail (Setaria viridis), quackgrass (Agropyron repens), Italian ryegrass (Lolium multiflorum) and ripgut brome (Bromus rigidus). The other pan was planted with seeds of Russian thistle (Salsola kali), tansy mustard (Descuraina pinnata), Galium aparine, tumble mustard (Sisymbrium altissium) kochia (Kochia scoparia), shepherd's purse (Capsella bursapastoris), Matricaria inodora, black nightshade (Solanum nigrum), yellow rocket (Barbarea vulgaris), wild mustard (Brassica kaber) and wild buckwheat (Polygonum convolvulus). In certain tests, rapeseed was substituted for wild mustard and Veronica persica was included. The above two pans were treated pre-emergence. At the same time two pans in which the above plant species were growing were treated post-emergence. Plant height at the time of treatment ranged from 1-15 cm depending on plant species.

The test compounds were diluted with a non-phytotoxic solvent and sprayed over-the-top of the pans. An untreated control and a solvent alone control were included for comparison. All treatments were maintained in the greenhouse for 20 days at which time the treatments were compared to the controls and the effects visually rated. The recorded data are presented in Table C. Several of the compounds tested exhibit utility for post-emergence weed control in wheat.

    TABLE C       Compound 1 Compound 35 Compound 35 Compound 43 Compound 46 Pre-Emergence       Post-Emergence Pre-Emergence Post-Emergence Pre-Emergence Post-Emergence       Pre-Emergence  Post-Emergence Rate kg/ha 0.015 0.06 0.015 0.06 0.25      0.06 0.015 0.004 0.25 0.06 0.015 0.004 0.25 0.06 0.25 0.06 0.015 0.004      0.015 0.004        wheat 0 0 2G 1C,3G 7G 5G 1G 0 7G 3G 1G 0 8G 0 7G 2G 4G 1G 6G 4G barley      0 0 4G 6G 8G -- 3G 0 8G 5G 1G 0 2G 2G 3C,5G 5G 8G 5G 8G 6G wild oats 0 0      2G 1G 6G 5G 2G 0 7G 5G 2G 0 5G 2G 2C,4G 2G 8G 5G 3C,8G 6G downy brome 0      2G 2G 3G 2C,9G 2C,8G 7G 5G 3C,9G 7G 7G 5G 8G 4G 4G 4G 9G 7G 3C,8G 8G      cheatgrass 0 1C,2G 6G 2C,8G 10E 10C 1C,8G 5G 2C,9G 8G 7G 5G 3C,8G 2G 4G      2G 2C,8G 6G 3C,8G 7G blackgrass 0 0 3G 2C,6G 4C,9G 2C,8G 3C,7G 5G 9C,9G      5C,9G 7C,8G 1C,5G 3C,8G 2H 8G 2C,5G 3C,9G 2C,8G 10C 3C,8G annual      bluegrass 0 2G 1C,4G 8C,9G 3C,9G 2C,8G 8G 4G 2C,8G 3C,8G 7G 3G 2C,8G 4G      4G 2G 4C,9G 2C,9G 9C,9G 3C,8G green foxtail 0 0 3G 5G 9G 5C,8G 2C,7G      3C,6G 2C,8G 2C,8G 1C,6G 3G 2C,5G 1C,2G 2C,7G 2C,4G 3C,9G 7G -- --      quackgrass 0 0 0 5G 2C,9G 2C,8G 8G 5G 1C,6G 1C,7G 6G 3G 5G 2G -- -- 9G      7G 6G 8G Italian ryegrass 0 1G 3G 9C,9G 10E 1C,8G 7G 1C,4G 2C,7G 8G 5G      2G 2C,8G 1C,2G 1C,2G 5G 4C,9G 7G 3C,8G 7G ripgut brome 0 0 2G 2C,6G      3C,9G 1C,8G 7G 4G 2C,8G 7G 5G 5G 2C,7G 2G 5G 2G 2C,8G 6G 2C,8G 6G      Russian thistle 0 0 3C,3G 4G 5C,7G 2C,6G 1C,3G 1C,3G 9C,9G 10C 7C,8G      5C,7G 1C 0 0 0 3G 0 0 0 tansy mustard 0 -- 9G 5G 9C,9G 7C,9G 2C,9G 9G      10C 10C 7C,8G 5C,7G 9C 9C 2C 1C,2G -- -- 10C 10C Galium aparine 0 0 2G      2G 3C,9G 7G 7G 6G 2C,7G 7G 4G -- 7C 3C 3C 3G 5G 5G 6G 3G tumble mustard      0 0 5G 10C 10C 5C,9G 9G 8G 10C 10C 10C 5C,8G 8G 4G 10C 6G 10C 9G 10C 10C      kochia 0 0 2G 4G 2C,9G 9G 8G 6G 10C 9C,9G 2C,7G 2C,2G 0 0 -- -- 8G 0 0      -- shepherd's purse 0 0 10C 2C,2G 10C 10C 2C,9G 9G 10C 10C 9C,9G 7C,9G      9G 8G 2C,2G 5G 10C 9G 10C 8G Matricaria inodora 0 0 3G 8C,8G 9G 9G 8G 7G      7C,9G 7C,8G 5C,9G 3C,8G 9G 6G 5G 1C,3G 9G 8G 2C,6G 3G black nightshade 0      0 0 0 3C,9G 8G 6G 4G 5C,8G 2C,7G 2C,7G 2G 5G 0 3C,8G 7G 9G 5G 2C,8G 6G      yellow rocket 0 0 0 0 3C,9G 9G 8G 8G 5C,9G 1C,7G 2G 0 9G 8G 7G 2G 9G 8G      8G 4G wild mustard 0 0 10C 9G 2C,9G 9G 1C,9G 7G 7C,8G 5C,9G 2C,7G 6G 9G      7G 8G 3G 9G 8G 6G 5G wild buckwheat 0 0 1G 0 2C,8G 8G 5G 2G 10C 6G 3G --      2G 0 5G 0 7G 5G 10C 2G Veronica persica                 -- -- 6G      4G

Test D

The test chemicals, dissolved in a non-phytotoxic solvent, were applied in an overall spray to the foliage and surrounding soil of selected plant species. One day after treatment, plants were observed for rapid burn injury. Approximately fourteen days after treatment, all species were visually compared to untreated controls and rated for response to treatment. The rating system was as described previously for Test A. The data are presented in Table D.

All plant species were seeded in Woodstown sandy loam soil and grown in a greenhouse. The following species were grown in soil contained in plastic pots (25 cm diameter by 13 cm deep): soybeans, cotton, alfalfa, corn, rice, wheat, sorghum, velvetleaf (Abutilon theophrasti), sesbania (Sesbania exaltata), sicklepod (Cassia obtusifolia), morningglory (Ipomoea hederacea), jimsonweed (Datura stramonium), cockelbur (Xanthium pensylvanicum), crabgrass (Digitaria sp.), nutsedge (Cyperus rotundus), barnyardgrass (Echinochloa crusgalli), giant foxtail (Setaria faberii) and wild oats (Avena fatua). The following species were grown in soil in a paper cup (12 cm diameter by 13 cm deep): sunflower, sugar beets, and mustard. All plants were sprayed approximately 14 days after planting. Additional plant species such as johnsongrass, rape and bindweed are sometimes added to this standard test in order to evaluate unusual selectivity.

Several of the compounds tested by this procedure exhibit post-emergence control of weeds in wheat, cotton and soybeans.

                                      TABLE D                                      __________________________________________________________________________             Compound 30                                                                            Compound 31                                                                               Compound 32 Compound 33                                                                            Compound 35                     Rate kg/ha                                                                             0.015                                                                              0.003                                                                              0.062                                                                              0.015                                                                              0.003                                                                             0.062                                                                              0.015                                                                              0.003                                                                              0.015                                                                              0.003                                                                              0.062                                                                             0.015                                                                             0.003                     __________________________________________________________________________     Soybeans                                                                               10G 7G,4C                                                                              7G  2G  0  8G  5G,4C                                                                              4C,4G                                                                              9C  8C  9C 9C 9C                        Velvetleaf                                                                             7G,6C                                                                              0   9G  5G  0  9G  5G,5C                                                                              3G  2C,8G                                                                              2G  9C 8G 6G                        Sesbania                                                                               9G  2G  9G  4G  2G 10C 9C  3C,4G                                                                              10C 8G,6C                                                                              10C                                                                               9G 8G                        Sicklepod                                                                              6G,3C                                                                              5G  2G  0   0  2C,5G                                                                              3G,2C                                                                              1C  1G  0   6G 0  0                         Cotton  9G  8G  5G  4G  0  4G,1C                                                                              4C,5G                                                                              3G,3C                                                                              2C  1C  10G                                                                               9G 9G                        Morningglory                                                                           0   6G  3G  2G  0  4G  4G  2G  0   0   9G 9G 8G                        Alfalfa 8G  9G  8G,2C                                                                              3G  8G 4G,3C                                                                              5G,3C                                                                              4G,2C                                                                              3G  2G  9G 9G 7G                        Jimsonweed                                                                             8G  0   3G  2G  0  3G  4G,3C                                                                              2G  2G  1C  9G 9G 7G                        Cocklebur                                                                              8G,3C                                                                              3C  6G  0   0  6G  4G  3G  --  5G  9G 8G 7G                        Corn    9G,8C                                                                              9G,8C                                                                              10G 10C 6G 10C 9C  6G,3C                                                                              1C,3G                                                                              2H,3G                                                                              10C                                                                               9G 8G                        Crabgrass                                                                              7G  0   3G  2G  0  4G  3G  1G  1G  0   9C 8G 4G                        Rice    9G,6C                                                                              3C,9G                                                                              8G,6C                                                                              8G,4C                                                                              8G 4G,4C                                                                              7G,5C                                                                              5G,3C                                                                              8C  6G,2C                                                                              9G 8G 8G                        Nutsedge                                                                               0   0   3G  2G  0  5G  3C,3G                                                                              1C,3G                                                                              3C,2G                                                                              0   9C 6C 2G                        Barnyardgrass                                                                          8G,6C                                                                              8G  7G,2C                                                                              6G  2G 10C 6G,3C                                                                              4G  3G  0   10C                                                                               9G 4G                        Wheat   5G  3G  6G  4G  2G 5G,4C                                                                              5G  3G  2G  0   6G 0  0                         Giant foxtail                                                                          9G,9C                                                                              9G  9G,6C                                                                              7G  4G 10C 8G  3G  7G  2G  10C                                                                               8G 6G                        Wild Oats                                                                              7G  5G  8G  4G  0  6G,3C                                                                              5G  4G  0   0   9G 5G 0                         Sorghum 8G  8G  10C 9G  5G 8C  9C  7G  7G  6G  9G 9G 6G                        Sunflower                                                                              10G 7G,3C                                                                              5G  0   0  10C 3G  3G  0   0   10C                                                                               8G 3G                        Rape    --  --  --  --  -- 8C  4C,7G                                                                              3C,5G                                                                              2G  1G  -- -- --                        Johnsongrass                                                                           10C 9G  9G,6U                                                                              7G  3G 10C 10C 4C,5G                                                                              4G,4C                                                                              0   9U 7G 0                         Sugar beets                                                                            8G  10C --  --  -- 10C 8C  7G,2C                                                                              2G,3C                                                                              1G,1C                                                                              9G 9G 7G                        Bindweed                                                                               0   0   0   0   0  8G  5G  2C,5G                                                                              0   1C  8G 4G 0                         Mustard 10C 7G,2C                                                                              10C 10C 9G --  --  --  --  --  9G 8G 3G                        __________________________________________________________________________             Compound 36                                                                             Compound 37                                                                            Compound 39                                                                            Compound 44                                                                               Compound 47                        Rate kg/ha                                                                             0.062                                                                               0.015                                                                              0.062                                                                              0.015                                                                              0.062                                                                              0.015                                                                              0.062                                                                               0.015                                                                             0.003                                                                             0.062                                                                              0.015                                                                              0.003                      __________________________________________________________________________     Soybeans                                                                               3C,5G                                                                               2C,5G                                                                              2C,1G                                                                              1G  6G,3C                                                                              6G  0    0  0  10G,7C                                                                             9G,4C                                                                              5G,4C                      Velvetleaf                                                                             1C   1G  0   1C  5G,2C                                                                              2G  6G   0  0  8C  6G  4G                         Sesbania                                                                               0    1G  0   0   9G  7G  6G   0  0  8G  5C  3C                         Sicklepod                                                                              2C   2C  2C,1G                                                                              1G  2G  2G  0    0  0  6C  5C  2C                         Cotton  5G,3C                                                                               4G,3C                                                                              2G  0   2G  0   9G   9G 2G 9G  9G  6G                         Morningglory                                                                           6G   5G  3C  0   6C,9G                                                                              7G,6C                                                                              3G   0  0  10G 8G  5G                         Alfalfa 3C   2G  2C  0   5G  0   2G   6G 0  8C,8G                                                                              4G  2C                         Jimsonweed                                                                             7G   6G  3G,2C                                                                              1C  3G  3G  0    0  0  7G  6G  2G                         Cocklebur                                                                              5C,8G                                                                               5G  3G  0   --  4G  9G   7G 0  10G 7G  3G                         Corn    8G   7G  1C,4G                                                                              1C,3G                                                                              9C,9G                                                                              3C,9G                                                                              8G,2H                                                                               5G 2G 8G,1H                                                                              6G,3H                                                                              0                          Crabgrass                                                                              0    0   1G  0   6G  2G  8G   5G 2G 6G  3G  0                          Rice    6G   5G  4G  4G  5G,2C                                                                              5G,4C                                                                              5G   2G 2G 9C  9G  4G                         Nutsedge                                                                               2G   0   2G  0   9G,5C                                                                              2G  0    0  0  8G  5G  0                          Barnyardgrass                                                                          0    0   0   0   9G,8C                                                                              7G  8G   8G 7G 9G  1H,9G                                                                              2G                         Wheat   0    0   2G  0   0   0   0    0  0  9G  9G  3G                         Giant foxtail                                                                          2G   1G  3G  0   6G  3G  4G   4G 4G 9C,9G                                                                              8G  4G                         Wild Oats                                                                              4G   1G  2G  0   0   0   4G   3G 0  9G  9G  2G                         Sorghum 8G   7G  8G  3G  7G  3G  8G   7G 3G 9G,4U                                                                              9G  9G                         Sunflower                                                                              6C,8G                                                                               4G  2C  0   7G,2C                                                                              7G,3C                                                                              8G   8G 0  10C 9G  5G                         Rape    5C,6G                                                                               4G,3C                                                                              4G,2C                                                                              2G  --  --  --   -- -- --  --  --                         Johnsongrass                                                                           3G   2G  2G,1C                                                                              1G  3G  0   8G   8G 8G 10U 10C 6G                         Sugar beets                                                                            2C,6G                                                                               1C,4G                                                                              1G  0   4G  4G  8G   8G 7G 9G  7G  0                          Bindweed                                                                               6G   3G  3C,2G                                                                              0   7G  9G  3G   3G 3G 8G  2G  0                          Mustard --   --  --  --  3G  3G  10C  7G 0  9G  8G  2G                         __________________________________________________________________________

Test E

For a greenhouse test, a set of 25-cm diameter plastic pots filled with Woodstown sandy loam were planted to Williams soybeans. Similar pots were used to plant the following weed species, three different species per pot: cocklebur (Xanthium pensylvanicum), sicklepod (Cassia obtusifolia), pitted morningglory (Ipomoea lacunosa), johnsongrass (Sorghum halepense), barnyarngrass (Echinochloa crusgalli) and giant foxtail (Setaria faberi). Immediately after planting, the pots were treated pre-emergence with Compound No. 30, dissolved in a non-phytotoxic solvent. The rates of application extended from 4 to 125 g/ha. The treated pots were held in the greenhouse for 27 days and the plants were then rated for response to the chemical treatments. The data are summarized in Table E. Note that Compound No. 30 has potential utility for weed control--particularly grass control--in soybeans.

    ______________________________________                                         Pre-emergence on Woodstown Sandy Loam                                          Compound No. 30                                                                           Percent Injury                                                      Rate (g/ha)  4      8     16   31   62   125  --                               ______________________________________                                         Cocklebur    10     40    70   90             0                                Sicklepod    0      20    20   10             0                                Pitted morningglory                                                                         0      20    50   60             0                                Johnsongrass 9o     90    90   95             0                                Barnyardgrass                                                                               0      20    60   95             0                                Giant foxtail                                                                               75     95    95   100            0                                Williams soybeans                   30   60                                    Untreated Control                                                                           0                 0    0    0    0                                ______________________________________                                     

What is claimed is:
 1. A compound of the formula: ##STR206## wherein X is CH₃, OCH₃, C₂ H₅ or OC₂ H₅ ;Z is N; Y is CH₂ OR, CH₂ S(O)_(m) R₁, CH(QR₁)₂, R₁ CHS(O)_(m) R₁, ##STR207## R is H, C(O)R₃, CO₂ R₄, C(O)NR₅ R₆ or ##STR208## R₁ is C₁ -C₂ alkyl; R₂ is --CH₂ CH₂ --, --CH(CH₃)CH₂ -- or --CH₂ CH₂ CH₂ --; R₃ is C₁ -C₃ alkyl; R₄ is C₁ -C₃ alkyl; R₅ is H or CH₃ ; R₆ is C₁ -C₃ alkyl; Q is O or S; m is 0, 1 or 2; A is ##STR209## R₇ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, I, Br, NO₂, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₂, S(O)_(n) R₁₃, LCF₃, LCHF₂, LCF₂ CF₂ H, CH₂ Cl, CHCl₂, CH₂ OCH₃ or CH₂ OCH₂ CH₃ ; R₈ is H, F, Cl, Br, CF₃, NO₂, C₁ -C₃ alkyl C₁ -C₃ alkoxy, OCF₂ H or SCF₂ H; R₉ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ Cl or CH₂ CH═CH₂ ; R₁₀ and R₁₁ are independently C₁ -C₃ alkyl; R₁₂ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ CH₂ OCH₃ or C₁ -C₄ alkyl substituted with 1-3 atoms of F, Cl or Br; R₁₃ is C₁ -C₄ alkyl or CH₂ CH═CH₂ ; n is 0 or 2; L is O, S or SO₂ ; R₁₄ is H, CH₃, OCH₃, F, Cl, Br, NO₂, SO₂ N(CH₃)₂, OSO₂ R₁ or S(O)_(n) R₁ ; R₁₅ is H, Cl, Br, CH₃, OCH₃ or NO₂ ; R₁₆ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ; R₁₇ is H, F, Cl, Br, CH₃ or OCH₃ ; W is O or S; W₁ is O or S; R₁₈ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, NO₂, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ; R₁₉ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, SO₂ NR₁₀ R₁₁, OSO₂ R₁₂, S(O)_(n) R₁₃, C₁ -C₃ alkyl, or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F; R₂₀ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, C₁ -C₃ alkyl, OSO₂ R₁₂ or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F; R₂₁ is H or CH₃ ;and their agriculturally suitable salts; provided that (1) the total number of carbon atoms of R₁₀ and R₁₁ is less than or equal to 4; (2) when W is O, then R₁₈ is H, Cl, Br, CH₃ or CO₂ R₉ ; (3) when W is O and R₁₈ is H, Cl, Br, or CH₃, then A is ##STR210## and (4) when W₁ is S, then R₂₁ is H and A is ##STR211##
 2. A compound of claim 1 where W₁ is O, X is CH₃, OCH₂ CH₃ or OCH₃ and R₂₁ is H.
 3. A compound of claim 2 where Y is CH(QR₁)₂, CH₂ SR₁, CR₁ (QR₁)₂, ##STR212##
 4. A compound of claim 3 where Y is CH(QR₁)₂, CH₂ SR₁ or ##STR213## and Q is
 0. 5. A compound of claim 4 whereinA is ##STR214## R₇ is C₁ -C₃ alkyl, C₁ -C₃ alkoxy, Cl, NO₂, CO₂ R₉, SO₂ (C₁ -C₃ alkyl), SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₃, CH₂ OCH₃ or LCF₂ H; R₁₄ is CH₃, OCH₃, Cl, OSO₂ CH₃ or SO₂ (C₁ -C₃ alkyl); R₁₆ is CH₃, OCH₃, Cl, SO₂ CH₃ or SO₂ N(CH₃)₂ ; R₁₈ is CH₃, Cl, Br, CO₂ R₉ or SO₂ CH₃.
 6. A compound of claim 5 where A is ##STR215##
 7. A compound of claim 6 whereR₇ is CO₂ CH₃, CO₂ CH₂ CH₃, SO₂ CH₃, SO₂ CH₂ CH₃, SO₂ N(CH₃)₂, OSO₂ CH₃, OSO₂ CH₂ CH₃ ; and R₈ is H, F, Cl, CF₃, CH₃ or OCH₃.
 8. The compound of claim 1 which is 2-[[[4-(hydroxymethyl)-6-methoxy-1,3,5-triazin-2-yl]-aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 9. The compound of claim 1 which is 2-[[[4-(dimethoxymethyl)-6-methoxy-1,3,5-triazin-2-yl]-aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 10. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 1 and at least one of the following: surfactant, solid or liquid inert diluent.
 11. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 2 and at least one of the following: surfactant, solid or liquid inert diluent.
 12. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 3 and at least one of the following: surfactant, solid or liquid inert diluent.
 13. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 4 and at least one of the following: surfactant, solid or liquid inert diluent.
 14. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 5 and at least one of the following: surfactant, solid or liquid inert diluent.
 15. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 6 and at least one of the following: surfactant, solid or liquid inert diluent.
 16. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 7 and at least one of the following: surfactant, solid or liquid inert diluent.
 17. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 8 and at least one of the following: surfactant, solid or liquid inert diluent.
 18. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 9 and at least one of the following: surfactant, solid or liquid inert diluent.
 19. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 1. 20. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 2. 21. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 3. 22. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 4. 23. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 5. 24. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 6. 25. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 7. 26. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 8. 27. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 9. 